Pyrazole-3-carboxylic acid amide derivative and pest control agent

ABSTRACT

Embodiments provide a harmful organism control agent containing a pyrazole-3-carboxylic acid amide derivative or a salt thereof as an active ingredient, having an excellent harmful organism controlling effect. A pyrazole-3-carboxylic acid amide derivative represented by general formula [I]: 
     
       
         
         
             
             
         
       
         
         
           
             (wherein, R 1 , R 2 , R 3 , R 4 , and R 5  represent a hydrogen atom, halogen atom, C 1 -C 6  alkyl group or the like, R 6  represents a C 1 -C 12  alkyl group, C 1 -C 12  haloalkyl group or the like, R 7  and R 8  represent a hydrogen atom, C 1 -C 12  alkyl group or the like) or an agriculturally acceptable salt thereof, and a harmful organism control agent containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof as an active ingredient.

CROSS REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of and priority to PCT/JP2018/018016, filed on May 9, 2018, entitled (translation), “PYRAZOLE-3-CARBOXYLIC ACID AMIDE DERIVATIVE AND PEST CONTROL AGENT,” which claims the benefit of and priority to Japanese Patent Application No. 2017-094998, filed on May 11, 2017, which are hereby incorporated by reference in their entirety into this application.

FIELD

The present invention relates to a novel pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof, and a harmful organism control agent containing the derivative as an active ingredient.

DESCRIPTION OF THE RELATED ART

Patent Document 1 discloses a pyrazole-3-carboxylic acid amide derivative having a harmful organism controlling effect, however, the compound disclosed in Patent Document 1 is limited to an oxazepine derivative in which the benzene ring substituting for the nitrogen atom of the carboxamide group at position 3 of the pyrazole ring, and the hydroxy group at position 4 form a ring.

Patent Documents 2 and 3 disclose a pyrazole-3-carboxylic acid amide derivative having an anticancer effect, however, the compounds disclosed in Patent Documents 2 and 3 are limited to derivatives in which a benzene ring and a pyridine ring substitute for the nitrogen atom of the carboxylic acid amide at position 3 of the pyrazole ring.

CITATION LIST Patent Documents

[Patent Document 1] WO 2016/027790 A

[Patent Document 2] WO 2012/028332 A

[Patent Document 3] WO 2016/166250 A

However, Patent Document 1 lacks description regarding a pyrazole-3-carboxylic acid amide derivative having a (substituted)alkoxy group at position 4 of the pyrazole ring. On the other hand, Patent Documents 2, 3 lack description regarding a pyrazole-3-carboxylic acid amide derivative in which a nitrogen atom in the carboxylic acid amide moiety at position 3 of the pyrazole ring is unsubstituted or has a (substituted)alkyl group. A harmful organism control agent used for useful crops are requested to be an agent that is applied to soil or foliage, and exhibits sufficient harmful organism controlling effect with a low dose. Also, increased demands for the safety and the influence on environment of chemicals lead to the request for developing a safer harmful organism control agent. Furthermore, in recent years, as a result of long-term use of a harmful organism control agent such as an insecticide or a miticide, harmful organisms having acquired the resistance to the harmful organism control agent have emerged, so that it becomes difficult to completely control harmful organisms. Also, use of harmful organism control agents having high mammalian toxicity is problematic in terms of the safety and the like for operators.

SUMMARY

In light of the aforementioned circumstance, it is an object of the present invention to solve the problems faced by the conventional harmful organism control agents, and to further provide a harmful organism control agent that is excellent in safety, control effect, residual activity, and the like.

In order to develop a harmful organism control agent having desirable characteristics as described above, the present inventors synthesized a variety of pyrazole-3-carboxylic acid amide derivatives, and diligently examined the physiological activity of the pyrazole-3-carboxylic acid amide derivatives. As a result, the present inventors found that a pyrazole-3-carboxylic acid amide derivative represented by the following general formula [I] (hereinafter, referred to as the present compound) shows outstanding effectiveness on various harmful organisms, and further continued the research to finally accomplish the present invention.

That is, the present invention has the subject matter having the following features.

(1) A pyrazole-3-carboxylic acid amide derivative represented by general formula [I] or an agriculturally acceptable salt thereof

wherein,

n represents an integer of 0 or 1,

X represents an oxygen atom or a sulfur atom,

R¹, R², R³, R⁴, and R⁵ each independently represent a hydrogen atom, halogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkoxy group, C₃-C₆ cycloalkyl group, C₁-C₆ alkylthio group, C₁-C₆ alkylsulfinyl group, C₁-C₆ alkylsulfonyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, cyano group, or nitro group,

R⁶ represents a hydrogen atom, C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)sulfonylamino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹,

R⁷ and R⁸ each independently represent a hydrogen atom, C₁-C₆ alkyl group, C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₂-C₇ alkynyl group, C₂-C₆ alkenyl group, hydroxy group, C₁-C₆ alkoxy group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, 2-tetrahydrofuranyl group, 3-tetrahydrofuranyl group, 2-tetrahydropyranyl group, 4-tetrahydropyranyl group, cyano C₁-C₆ alkyl group, cyano C₃-C₆ cycloalkyl group, hydroxy C₁-C₆ alkyl group, formyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, C₁-C₆ alkylcarbonyl group, C₁-C₆ alkoxy C₁-C₆ alkylcarbonyl group, C₃-C₆ cycloalkyl carbonyl group, C₃-C₆ cycloalkyl C₁-C₆ alkylcarbonyl group, C₁-C₆ alkoxycarbonyl group, carbamoyl group, mono(C₁-C₆ alkyl)aminocarbonyl group, di(C₁-C₆ alkyl)aminocarbonyl group, phenylcarbonyl group that is unsubstituted or substituted with R⁹, C₇-C₁₃ aralkylcarbonyl group that is unsubstituted or substituted with R⁹, pyridylcarbonyl group that is unsubstituted or substituted with R⁹, pyrazolylcarbonyl group that is unsubstituted or substituted with R⁹, (C₁-C₆ alkyl)thiocarbonyl group, (C₁-C₆ alkoxy)thiocarbonyl group, thiocarbamoyl group, mono(C₁-C₆ alkyl)aminothiocarbonyl group, di(C 1-C₆ alkyl)aminothiocarbonyl group, C 1-C₆ alkylsulfonyl group, sulfamoyl group, mono(C₁-C₆ alkyl)aminosulfonyl group, di(C₁-C₆ alkyl)aminosulfonyl group, R¹⁰R¹¹N—C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, hydroxyimino group, C₁-C₆ alkoxyimino group, hydroxyimino C₁-C₆ alkyl group, or C₁-C₆ alkoxyimino C₁-C₆ alkyl group, and R⁷ and R⁸ may together form ═CR¹²N(R¹³)R¹⁴ or ═CR¹²OR¹⁵, and R⁷ and R⁸ may form, together with a carbon atom bound thereto, a 3 to 6-membered carbon ring, or a 3 to 6-membered hetero ring having 1 to 4 heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and the hetero ring may be substituted with a halogen atom, cyano group, nitro group, C₁-C₆ alkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkyl group, or oxo group,

R⁹ represents a halogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkoxy group, C₁-C₆ alkylthio group, C₁-C₆ alkylsulfinyl group, C₁-C₆ alkylsulfonyl group, C₁-C₆ haloalkylthio group, C₁-C₆ haloalkylsulfinyl group, C₁-C₆ haloalkylsulfonyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, cyano group, or nitro group,

R¹⁰ and R¹¹ each independently represent a hydrogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, or C₃-C₆ cycloalkyl group, and R¹⁰ and R¹¹ may form, together with a carbon atom bound thereto, a 3 to 6-membered ring,

R¹² represents a hydrogen atom, C₁-C₆ alkyl group, or C₃-C₆ cycloalkyl group,

R¹³ and R¹⁴ each independently represent a hydrogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₃-C₆ cycloalkyl group, or C₁-C₆ alkoxy group, and R¹³ and R¹⁴ may form, together with a carbon atom bound thereto, a 3 to 6-membered carbon ring, or a 3 to 6-membered hetero ring having 1 to 4 heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and

R¹⁵ represents a C₁-C₆ alkyl group.

(2) A pyrazole-3-carboxylic acid derivative represented by general formula [II] or a salt thereof

wherein,

n represents an integer of 0 or 1,

R¹, R², R³, R⁴, and R⁵ each independently represent a hydrogen atom, halogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkoxy group, C₃-C₆ cycloalkyl group, C₁-C₆ alkylthio group, C₁-C₆ alkylsulfinyl group, C₁-C₆ alkylsulfonyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, cyano group, or nitro group,

R⁶ represents a hydrogen atom, C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)carbonylamino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxy)carbonylamino C₁-C₆ alkyl group, mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl sulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹, and

R¹⁶ represents a hydrogen atom or C₁-C₆ alkyl group.

(3) The pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to (1), wherein R⁶ represents a C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)carbonylamino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxy)carbonylamino C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)sulfonylamino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)sulfonylamino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹.

(4) The pyrazole-3-carboxylic acid derivative or a salt thereof according to (2), wherein R⁶ represents a C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)carbonylamino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxy)carbonylamino C₁-C₆ alkyl group, mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or a C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹.

(5) A pesticide composition containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to (1) or (3), or the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to (2) or (4) as an active ingredient.

(6) The pesticide composition according to (5), wherein the pesticide composition further contains a surfactant.

(7) A harmful organism control agent containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to (1) or (3), or the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to (2) or (4) as an active ingredient.

(8) The harmful organism control agent according to (7) that is an insecticide.

(9) The harmful organism control agent according to (7) having a control effect on a harmful organism in a dry field or a paddy field where a farming or gardening plant is cultured.

(10) The harmful organism control agent according to (9), wherein the farming or gardening plant is a plant provided with tolerance by a breeding method or a gene recombination technique.

(11) A method for controlling a harmful organism using an active ingredient amount of the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to (1) or (3), or the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to (2) or (4).

(12) A method for controlling a harmful organism by letting a pesticide composition containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to (1) or (3), or the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to (2) or (4) as an active ingredient act on a farming or gardening crop or a place where the farming or gardening crop is to be grown or being grown, at once or in batch.

(13) The method for controlling a harmful organism according to (11) or (12), wherein the place where the harmful organism control agent is to be applied is a paddy field, a dry field, a lawn, an orchard, a non-crop land, a greenhouse, a raising seeding facility, or a plant factory.

(14) The method for controlling a harmful organism according to any one of (11) to (13), wherein the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof is used as an insecticide.

(15) A use method of a harmful organism control agent, using the harmful organism control agent according to any one of (7) to (10) for controlling a harmful organism for a farming or gardening crop.

The harmful organism control agent containing the present compound shows excellent controlling effect on a wide range of harmful organisms including Hemiptera pests, Lepidoptera pests, Coleoptera pests, Diptera pests, Hymenoptera pests, Orthoptera pests, Isoptera pests, Thysanoptera pests, Acari pests, and plant parasitic nematoda, and is capable of controlling a harmful organism having acquired drug resistance.

DETAILED DESCRIPTION

Symbols and terms used in this specification are described.

In the present invention, “harmful organism control agent” means insecticides, miticides, nematicides, and the like in farming and gardening fields, for animals such as domestic animals and pets, for household use or for prevention of epidemics.

In the present invention, “halogen atom” refers to a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom.

In the present invention, the notation “C₁-C₆” and the like indicates that the number of carbons in the substituent following the notation is 1 to 6, in this case.

In the present invention, unless otherwise specified, “C₁-C₆ alkyl group” refers to a linear or branched alkyl group having 1 to 6 carbon atoms, and examples of the C₁-C₆ alkyl group include a methyl, ethyl, n-propyl, isopropyl, n-butyl, s-butyl, isobutyl, tert-butyl, n-pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1-ethylpropyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, neopentyl, n-hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1-ethylbutyl, 2-ethylbutyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl, or 1-ethyl-2-methylpropyl group.

In the present invention, unless otherwise specified, “C₁-C₁₂ alkyl group” refers to a linear or branched alkyl group having 1 to 12 carbon atoms, and examples of the C₁-C₁₂ alkyl group include, in addition to those exemplified in the “C₁-C₆ alkyl group”, a n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, 4,4-dimethylpentyl, 5-methylhexyl, 5,5-dimethylhexyl, 3,5,5-trimethylhexyl, 6-methylheptyl, 6,6-dimethylheptyl, 3,6,6-trimethylheptyl, 7-methyloctyl, 7,7-dimethyloctyl, 8-methylnonyl, 8,8-dimethylnonyl, 9-methyldecyl, 9,9-dimethyldecyl or 10-methylundecyl group.

In the present invention, unless otherwise specified, “C₂-C₆ alkenyl group” refers to a linear or branched alkenyl group having 2 to 6 carbon atoms, and examples of the C₂-C₆ alkenyl group include a vinyl, 1-propenyl, isopropenyl, 2-propenyl, 1-butenyl, 1-methyl-1-propenyl, 2-butenyl, 1-methyl-2-propenyl, 3-butenyl, 2-methyl-1-propenyl, 2-methyl-2-propenyl, 1,3-butadienyl, 1-pentenyl, 1-ethyl-2-propenyl, 2-pentenyl, 1-methyl-1-butenyl, 3-pentenyl, 1-methyl-2-butenyl, 4-pentenyl, 1-methyl-3-butenyl, 3-methyl-1-butenyl, 1,2-dimethyl-2-propenyl, 1,1-dimethyl-2-propenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1,2-dimethyl-1-propenyl, 2-methyl-3-butenyl, 3-methyl-3-butenyl, 1,3-pentadienyl, 1-vinyl-2-propenyl, 1-hexenyl, 1-propyl-2-propenyl, 2-hexenyl, 1-methyl-1-pentenyl, 1-ethyl-2-butenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-4-pentenyl, 1-ethyl-3-butenyl, 1-(isobutyl)vinyl, 1-ethyl-1-methyl-2-propenyl, 1-ethyl-2-methyl-2-propenyl, 1-(isopropyl)-2-propenyl, 2-methyl-2-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1,3-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1,5-hexadienyl, 1-vinyl-3-butenyl, or 2,4-hexadienyl group.

In the present invention, unless otherwise specified, “C₂-C₇ alkynyl group” refers to a linear or branched alkynyl group having 2 to 7 carbon atoms, and examples of the C₂-C₇ alkynyl group include an ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 1-methyl-2-propynyl, 2-butynyl, 3-butynyl, 1-pentynyl, 1-ethyl-2-propynyl, 2-pentynyl, 3-pentynyl, 1-methyl-2-butynyl, 4-pentynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 1-hexynyl, 1-(n-propyl)-2-propynyl, 2-hexynyl, 1-ethyl-2-butynyl, 3-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 4-methyl-1-pentynyl, 3-methyl-1-pentynyl, 5-hexynyl, 1-ethyl-3-butynyl, 1-ethyl-1-methyl-2-propynyl, 1-(isopropyl)-2-propynyl, 1,1-dimethyl-2-butynyl or 2,2-dimethyl-3-butynyl, 1-heptynyl, 1-(n-butyl)-2-propynyl, 1-(s-butyl)-2-propynyl, 1-isobutyl-2-propynyl, 2-heptynyl, 3-heptynyl, 1-methyl-2-hexynyl, 4-methyl-2-hexynyl, 5-methyl-2-hexynyl, 6-heptynyl, 1,1-diethyl-2-propynyl, 1-methyl-1-propyl-2-propynyl, 1-isopropyl-1-methyl-2-propynyl, 1,1-dimethyl-2-pentynyl, 1,4-dimethyl-2-pentynyl, or 4,4-dimethyl-2-pentynyl group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkyl group” refers to a linear or branched alkynyl group having 1 to 6 carbon atoms, substituted with the same or different 1 to 13 halogen atoms, for example, a haloalkyl group, and examples of the C₁-C₆ haloalkyl group include a fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, bromomethyl, dibromomethyl, tribromomethyl, iodomethyl, chlorodifluoromethyl, dichlorofluoromethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, pentafluoroethyl, 1-chloroethyl, 2-chloroethyl, 1,1-dichloroethyl, 2,2-dichloroethyl, 2,2,2-trichloroethyl, 1,1,2,2-tetrachloroethyl, pentachloroethyl, 1-bromoethyl, 2-bromoethyl, 2,2,2-tribromoethyl, 1-iodoethyl, 2-iodoethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro-2-fluoroethyl, 1-fluoropropyl, 2-fluoropropyl, 3-fluoropropyl, 1,1-difluoropropyl, 2,2-difluoropropyl, 3,3-difluoropropyl, 3,3,3-trifluoropropyl, 2,2,3,3,3-pentafluoropropyl, 1,1,2,3,3,3-hexafluoropropyl, heptafluoropropyl, 1-fluoropropane-2-yl, 2-fluoropropane-2-yl, 1,1-difluoropropane-2-yl, 1,2-difluoropropane-2-yl, 1,3-difluoropropane-2-yl, 1,2,3-trifluoropropane-2-yl, 1,1,3,3-tetrafluoropropane-2-yl, 1,1,1,3,3,3-hexafluoropropane-2-yl, heptafluoropropane-2-yl, 1-chloropropyl, 2-chloropropyl, 3-chloropropyl, 1,1-dichloropropyl, 2,2-dichloropropyl, 3,3-dichloropropyl, 3,3,3-trichloropropyl, 2,2,3,3,3-pentachloropropyl, heptachloropropyl, 1-chloropropane-2-yl, 2-chloropropane-2-yl, 1,1-dichloropropane-2-yl, 1,2-dichloropropane-2-yl, 1,3-dichloropropane-2-yl, 1,2,3-trichloropropane-2-yl, 1,1,3,3-tetrachloropropane-2-yl, 1,1,1,3,3,3-hexachloropropane-2-yl, heptachloropropane-2-yl, 1-bromopropyl, 2-bromopropyl, 3-bromopropyl, 1-bromopropane-2-yl, 2-bromopropane-2-yl, 1-iodopropyl, 2-iodopropyl, 3-iodopropyl, 1-iodopropane-2-yl, 2-iodopropane-2-yl, 1-fluorobutyl, 2-fluorobutyl, 3-fluorobutyl, 4-fluorobutyl, 4,4-difluorobutyl, 4,4,4-trifluorobutyl, 4,4,4-trifluoro-3-methylbutyl, 3,3,4,4,4-pentafluorobutyl, 2,2,3,4,4,4-hexafluorobutyl, 2,2,3,3,4,4,4-heptafluorobutyl, nonafluorobutyl, 1,1,1-trifluorobutane-2-yl, 4,4,4-trifluorobutane-2-yl, 3,3,4,4,4-pentafluorobutane-2-yl, nonafluorobutane-2-yl, 1,1,1,3,3,3-hexafluoro-2-(trifluoromethyl)propane-2-yl, 1-chlorobutyl, 2-chlorobutyl, 3-chlorobutyl, 4-chlorobutyl, 4,4-dichlorobutyl, 4,4,4-trichlorobutyl, nonachlorobutyl, 1,1,1-trichlorobutane-2-yl, 4,4,4-trichlorobutane-2-yl, nonachlorobutane-2-yl, 1-bromobutyl, 2-bromobutyl, 3-bromobutyl, 4-bromobutyl, 1-iodobutyl, 2-iodobutyl, 3-iodobutyl, 4-iodobutyl, 4-chloro-1,1,2,2,3,3,4,4-octafluorobutyl, 4-bromo-1,1,2,2,3,3,4,4-octafluorobutyl, 1-fluoropentyl, 2-fluoropentyl, 3-fluoropentyl, 4-fluoropentyl, 5-fluoropentyl, 5,5,5-trifluoropentyl, 4,4,5,5,5-pentafluoropentyl, 3,3,4,4,5,5,5-heptafluoropentyl, 2,2,3,3,4,4,5,5-octafluoropentyl, 2,2,3,3,4,4,5,5,5-nonafluoropentyl, undecafluoropentyl, 1-chloropentyl, 2-chloropentyl, 3-chloropentyl, 4-chloropentyl, 5-chloropentyl, 5,5,5-trichloropentyl, 4,4,5,5,5-pentachloropentyl, 3,3,4,4,5,5,5-heptachloropentyl, 2,2,3,3,4,4,5,5,5-nonachloropentyl, undecachloropentyl, 1-bromopentyl, 2-bromopentyl, 3-bromopentyl, 4-bromopentyl, 5-bromopentyl, 5-iodopentyl, 1-fluorohexyl, 2-fluorohexyl, 3-fluorohexyl, 4-fluorohexyl, 5-fluorohexyl, 6-fluorohexyl, 6,6,6-trifluorohexyl, 5,5,6,6,6-pentafluorohexyl, 4,4,5,5,6,6,6-heptafluorohexyl, 3,3,4,4,5,5,6,6,6-nonafluorohexyl, 2,2,3,3,4,4,5,5,6,6,6-undecafluorohexyl, 2,2,3,3,4,4,5,5,6,6-decafluorohexyl, tridecafluorohexyl, 1-chlorohexyl, 2-chlorohexyl, 3-chlorohexyl, 4-chlorohexyl, 5-chlorohexyl, 6-chlorohexyl, 5-bromohexyl, 6-bromohexyl, 5-iodohexyl, or 6-iodohexyl group.

In the present invention, unless otherwise specified, “C₁-C₁₂ haloalkyl group” refers to a linear or branched alkyl group having 1 to 12 carbon atoms, substituted with the same or different 1 to 25 halogen atoms, and examples of the C₁-C₁₂ haloalkyl group include, in addition to those exemplified in the “C₁-C₆ haloalkyl group”, a 2,2,3,4,4,6,6,6-octafluoro-3,5,5-tris(trifluoromethyl)hexyl, 7,7,7-trifluoroheptyl, 1H,1H-perfluoroheptyl, 1H,1H,2H,2H-perfluoroheptyl, 1H, 1H,2H,2H,3H,3H-perfluoroheptyl, 1H,1H,7H-perfluoroheptyl, perfluoroheptyl,2-(perfluoro-3-methylbutyl)ethyl, 1H,1H-perfluorooctyl, 1H,1H,2H,2H-perfluorooctyl, 1H,1H,2H,2H,3H,3H-perfluorooctyl, 6-(perfluorohexyl)ethyl, 1H,1H,8H-perfluorooctyl, perfluorooctyl, 1H,1H-perfluorononyl, 1H,1H,2H,2H-perfluorononyl, 1H,1H,2H,2H,3H,3H-perfluorononyl, 6-(perfluoro-1-methylethyl)hexyl, 1H,1H,9H-perfluorononyl, perfluorononyl, 1H,1H-perfluorodecyl, 1H,1H,2H,2H-perfluorodecyl, 1H,1H,2H,2H,3H,3H-perfluorodecyl, 6-(perfluorobutyl)hexyl, 1H,1H,9H-perfluorodecyl, or perfluorodecyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkoxy group” refers to a (C₁-C₆ alkyl)-O— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkoxy group include a methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, 1-methylbutoxy, 2-methylbutoxy, 3-methylbutoxy, 1-ethylpropoxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, or n-hexyloxy group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkoxy group” refers to a (C₁-C₆ haloalkyl)-O— group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkoxy group include a difluoromethoxy, dichloromethoxy, trifluoromethoxy, trichloromethoxy, tribromomethoxy, chlorodifluoromethoxy, bromodifluoromethoxy, 2-fluoroethoxy, 1-chloroethoxy, 2-chloroethoxy, 1-bromoethoxy, 2-bromoethoxy, 2,2-difluoroethoxy, 1,2-dichloroethoxy, 2,2-dichloroethoxy, 2,2,2-trifluoroethoxy, 2,2,2-trichloroethoxy, 1,1,2,2-tetrafluoroethoxy, pentafluoroethoxy, 2-bromo-2-chloroethoxy, 2-chloro-1,1,2,2-tetrafluoroethoxy, 1-chloro-1,2,2,2-tetrafluoroethoxy, 1-chloropropoxy, 2-chloropropoxy, 3-chloropropoxy, 2-bromopropoxy, 3-bromopropoxy, 2-bromo-1-methylethoxy, 3-iodopropoxy, 2,3-dichloropropoxy, 2,3-dibromopropoxy, 3,3,3-trifluoropropoxy, 3,3,3-trifluoro-2-propoxy, 3,3,3-trichloropropoxy, 3-bromo-3,3-difluoropropoxy, 2,2-difluoropropoxy, 3,3-dichloro-3-fluoropropoxy, 2,2,3,3-tetrafluoropropoxy, 1-bromo-3,3,3-trifluoropropoxy, 2,2,3,3,3-pentafluoropropoxy, 2,2,2-trifluoro-1-trifluoromethylethoxy, heptafluoropropoxy, heptafluoro-2-propoxy, 1,2,2,2-tetrafluoro-1-trifluoromethylethoxy, 1,1,2,3,3,3-hexafluoropropoxy, 2-chlorobutoxy, 3-chlorobutoxy, 4-chlorobutoxy, 2-chloro-1,1-dimethylethoxy, 4-bromobutoxy, 3-bromo-2-methylpropoxy, 2-bromo-1,1-dimethylethoxy, 2,2-dichloro-1,1-dimethylethoxy, 2-chloro-1-chloromethyl-2-methylethoxy, 4,4,4-trifluorobutoxy, 3,3,3-trifluoro-1-methylpropoxy, 3,3,3-trifluoro-2-methylpropoxy, 2,3,4-trichlorobutoxy, 2,2,2-trichloro-1,1-dimethylethoxy, 4-chloro-4,4-difluorobutoxy, 4,4-dichloro-4-fluorobutoxy, 4-bromo-4,4-difluorobutoxy, 2,4-dibromo-4,4-difluorobutoxy, 3,4-dichloro-3,4,4-trifluorobutoxy, 3,3-dichloro-4,4,4-trifluorobutoxy, 4-bromo-3,3,4,4-tetrafluorobutoxy, 4-bromo-3-chloro-3,4,4-trifluorobutoxy, 2,2,3,3,4,4-hexafluorobutoxy, 2,2,3,4,4,4-hexafluorobutoxy, 2,2,2-trifluoro-1-methyl-1-trifluoromethylethoxy, 3,3,3-trifluoro-2-trifluoromethylpropoxy, 2,2,3,3,4,4,4-heptafluorobutoxy, 3,3,4,4,4-pentafluoro-2-butoxy, 2,3,3,3-tetrafluoro-2-trifluoromethylpropoxy, 1,1,2,2,3,3,4,4-octafluorobutoxy, nonafluorobutoxy, perfluoro-tert-butoxy, 4-chloro-1,1,2,2,3,3,4,4-octafluorobutoxy, 5,5,5-trifluoropentoxy, 4,4,5,5,5-pentafluoropentoxy, 3,3,4,4,5,5,5-heptafluoropentoxy, 3,3,4,4,5,5,5-heptafluoro-2-pentoxy, 2,2,3,3,4,4,5,5,5-nonafluoropentoxy, 2,2,3,3,4,4,5,5-octafluoropentoxy, perfluoropentoxy, 4,4,5,5,5-pentafluoro-2-butoxy, 2,2-bis(trifluoromethyl)propoxy, 2,2,3,3,4,4,5,5,6,6,6-undecafluorohexyloxy, 3,3,4,4,5,5,6,6,6-nonafluorohexyloxy, 4,4,5,5,6,6,6-heptafluorohexyloxy, 2,2,3,3,4,4,5,5,6,6-decafluorohexyloxy, 4,4,4-trifluoro-3,3-bis(trifluoromethyl)butyloxy, or perfluorohexyloxy group.

In the present invention, unless otherwise specified, “C₃-C₆ cycloalkyl group” refers to a cycloalkyl group having 3 to 6 carbon atoms, and examples of the C₃-C₆ cycloalkyl group include a cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl group.

In the present invention, unless otherwise specified, “C₃-C₆ cycloalkyl C₂-C₆ alkynyl group” refers to a (C₃-C₆ cycloalkyl)-(C₂-C₆ alkynyl)- group in which the cycloalkyl moiety is as defined above, and examples of the C₃-C₆ cycloalkyl C₂-C₆ alkynyl group include a 3-cyclopropyl-2-propynyl, 3-cyclobutyl-2-propynyl, 3-cyclopentyl-2-propynyl, 3-cyclohexyl-2-propynyl, 3-cyclopropyl-1-methyl-2-propynyl, 3-cyclobutyl-1-methyl-2-propynyl, 3-cyclopentyl-1-methyl-2-propynyl or 3-cyclohexyl-1-methyl-2-propynyl group.

In the present invention, “C₁-C₆ alkylthio group” refers to a (C₁-C₆ alkyl)-S— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylthio group include a methylthio, ethylthio, n-propylthio, isopropylthio, n-butylthio, isobutylthio, sec-butylthio, or tert-butylthio group.

In the present invention, “C₁-C₆ alkylsulfinyl group” refers to a (C₁-C₆ alkyl)-SO— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylsulfinyl group include a methylsulfinyl, ethylsulfinyl, n-propylsulfinyl, isopropylsulfinyl, n-butylsulfinyl, isobutylsulfinyl, sec-butylsulfinyl, or tert-butylsulfinyl group.

In the present invention, “C₁-C₆ alkylsulfonyl group” refers to a (C₁-C₆ alkyl)-SO₂— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylsulfonyl group include a methylsulfonyl, ethylsulfonyl, n-propylsulfonyl, isopropylsulfonyl, n-butylsulfonyl, isobutylsulfonyl, sec-butylsulfonyl, or tert-butylsulfonyl group.

In the present invention, “mono(C₁-C₆ alkyl)amino group” refers to a (C₁-C₆ alkyl)-NH— group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkyl)amino group include a methylamino, ethylamino, n-propylamino, or isopropyl amino group.

In the present invention, “di(C₁-C₆ alkyl)amino group” refers to a (C₁-C₆ alkyl)₂-N— group in which the alkyl moiety is as defined above, and examples of the di(C₁-C₆ alkyl)amino group include a dimethylamino, diethylamino, or N-ethyl-N-methylamino group.

In the present invention, “C₁-C₆ alkoxy C₁-C₆ alkyl group” refers to a (C₁-C₆ alkoxy)-(C₁-C₆ alkyl)- group in which the alkoxy moiety is as defined above, and examples of the C₁-C₆ alkoxy C₁-C₆ alkyl group include a methoxymethyl, 1-methoxyethyl, 2-methoxyethyl, 2-ethoxyethyl, 2-methoxypropyl, 3-methoxypropyl, 2-ethoxypropyl, 3-ethoxypropyl, 1-methyl-3-methoxybutyl, or 3-butoxybutyl group.

In the present invention, “C₁-C₆ alkoxy C₁-C₆ haloalkyl group” refers to a (C₁-C₆ alkoxy)-(C₁-C₆ haloalkyl)- group in which the alkoxy moiety is as defined above, and examples of the C₁-C₆ alkoxy C₁-C₆ haloalkyl group include a 2-methoxy-1,1,2-trifluoroethyl or 2-ethoxy-1,1,2-trifluoroethyl group.

In the present invention, “C₁-C₆ haloalkoxy C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkoxy)-(C₁-C₆ alkyl)- group in which the haloalkoxy moiety is as defined above, and examples of the C₁-C₆ haloalkoxy C₁-C₆ alkyl group include a 2-(difluoromethoxy)ethyl, 2-(trifluoromethoxy)ethyl, 2-(2,2-difluoroethoxy)ethyl, or 2-(2,2,2-trifluoroethoxy)ethyl group.

In the present invention, “C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group” refers to a (C₁-C₆ haloalkoxy)-(C₁-C₆ haloalkyl)- group in which the haloalkoxy moiety is as defined above, and examples of the C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group include a 1,1,2-trifluoro-2-(trifluoromethoxy)ethyl, 1,1,2-trifluoro-2-(pentafluoroethoxy)ethyl, or 1,1,2-trifluoro-2-(heptafluoropropoxy)ethyl group.

In the present invention, unless otherwise specified, “C₂-C₆ haloalkynyl group” refers to a linear or branched alkynyl group having 2 to 6 carbon atoms, substituted with the same or different 1 to 9 halogen atoms, and examples of the C₂-C₆ haloalkynyl group include a fluoroethynyl, chloroethynyl, bromoethynyl, iodoethynyl, 3-fluoro-2-propynyl, 3-chloro-2-propynyl, 3-bromo-2-propynyl, 3-iodo-2-propynyl, 4-fluoro-3-butynyl, 4-chloro-3-butynyl, 4-bromo-3-butynyl, 4-iodo-3-butynyl, 4,4-difluoro-2-butynyl, 4,4-dichloro-2-butynyl, 4,4,4-trifluoro-2-butynyl, 4,4,4-trichloro-2-butynyl, 3-fluoro-1-methyl-2-propynyl, 3-chloro-1-methyl-2-propynyl, 5-fluoro-4-pentynyl, 5-chloro-4-pentynyl, 5,5,5-trifluoro-3-pentynyl, 5,5,5-trichloro-3-pentynyl, 4-fluoro-2-methyl-3-butynyl, 4-chloro-2-methyl-3-butynyl, 6-fluoro-5-hexynyl, 6-chloro-5-hexynyl, 6,6,6-trifluoro-4-hexynyl, 6,6,6-trichloro-4-hexynyl, 5-fluoro-3-methyl-4-pentynyl, or 5-chloro-3-methyl-4-pentynyl group.

In the present invention, unless otherwise specified, “C₂-C₆ haloalkenyl group” refers to a linear or branched alkenyl group having 2 to 6 carbon atoms, substituted with the same or different 1 to 11 halogen atoms, and examples of the C₂-C₆ haloalkenyl group include a 1-fluorovinyl, 2-fluorovinyl, 1,2-difluorovinyl, 2,2-difluorovinyl, trifluorovinyl, 1-chlorovinyl, 2-chlorovinyl, 1,2-dichlorovinyl, 2,2-dichlorovinyl, trichlorovinyl, 1,2-dibromovinyl, 2,2-dibromovinyl, tribromovinyl, 1,2-diiodovinyl, 2,2-diiodovinyl, triodovinyl, 1-fluoro-2-propenyl, 2-fluoro-2-propenyl, 3-fluoro-2-propenyl, 2,3-difluoro-2-propenyl, 3,3-difluoro-2-propenyl, 3,3-difluoro-1-propenyl, 2,3,3-trifluoro-2-propenyl, 3,3,3-trifluoro-1-propenyl, 2-chloro-3,3,3-trifluoro-1-propenyl, 1,2,3,3,3-pentafluoro-1-propenyl, 1-chloro-2-propenyl, 2-chloro-2-propenyl, 3-chloro-2-propenyl, 2,3-dichloro-2-propenyl, 3,3-dichloro-2-propenyl, 3,3-dichloro-1-propenyl, 2,3,3-trichloro-2-propenyl, 3,3,3-trichloro-1-propenyl, 3-bromo-2-propenyl, 3,3-dibromo-2-propenyl, 3,3-diiodo-2-propenyl, 2,2-difluoro-1-propene-2-yl, 3,3,3-trifluoro-1-propene-2-yl, 3,3,3-trichloro-1-propene-2-yl, 4-fluoro-3-butenyl, 4,4-difluoro-3-butenyl, 4,4-difluoro-3-butene-2-yl, 4,4,4-trifluoro-2-butenyl, 3,4,4-trifluoro-3-butenyl, 2-trifluoromethyl-2-propenyl, 2-trifluoromethyl-3,3-difluoro-2-propenyl, 4,4,4-trifluoro-3-chloro-2-butenyl, 4,4-dichloro-3-butenyl, 4,4,4-trichloro-2-butenyl, 2-trichloromethyl-2-propenyl, 5,5-difluoro-4-pentenyl, 4,5,5-trifluoro-4-pentenyl, 5,5,5-trifluoro-3-pentenyl, 4,4,4-trifluoro-3-methyl-2-butenyl, 4,4,4-trifluoro-3-trifluoromethyl-2-butenyl, 5,5-dichloro-4-pentenyl, 4,4,4-trichloro-3-methyl-2-butenyl, 6,6-difluoro-5-hexenyl, 5,6,6-trifluoro-5-pentenyl, 6,6,6-trifluoro-4-pentenyl, 5,5,5-trifluoro-4-methyl-3-pentenyl, 5,5,5-trifluoro-4-trifluoromethyl-3-pentenyl, 6,6-dichloro-5-hexenyl, or 5,5,5-trichloro-4-methyl-3-pentenyl group.

In the present invention, unless otherwise specified, “C₃-C₆ halocycloalkyl group” refers to a cycloalkyl group having 3 to 6 carbon atoms, substituted by the same or different 1 to 11 halogen atoms, and examples of the C₃-C₆ halocycloalkyl group include a 1-fluorocyclopropyl, 2-fluorocyclopropyl, 2,2-difluorocyclopropyl, 2,2,3,3-tetrafluorocyclopropyl, 1-chlorocyclopropyl, 2-chlorocyclopropyl, 2,2-dichlorocyclopropyl, 2,2,3,3-tetrachlorocyclopropyl, 2,2-dibromocyclopropyl, 2,2-diiodocyclopropyl, 1-fluorocyclobutyl, 2-fluorocyclobutyl, 3-fluorocyclobutyl, 3,3-difluorocyclobutyl, heptafluorocyclobutyl, 2-chlorocyclobutyl, 3-chlorocyclobutyl, 3,3-dichlorocyclobutyl, 3,3-dibromocyclobutyl, 3,3-diiodocyclobutyl, 1-fluorocyclopentyl, 2-fluorocyclopentyl, 3-fluorocyclopentyl, 2,2-difluorocyclopentyl, 3,3-difluorocyclopentyl, nonafluorocyclopentyl, 2,2-dichlorocyclopentyl, 3,3-dichlorocyclopentyl, 2,2-dibromocyclopentyl, 3,3-dibromocyclopentyl, 2,2-diiodocyclopentyl, 3,3-diiodocyclopentyl, 1-fluorocyclohexyl, 2-fluorocyclohexyl, 3-fluorocyclohexyl, 4-fluorocyclohexyl, 2,2-difluorocyclohexyl, 3,3-difluorocyclohexyl, 4,4-difluorocyclohexyl, 1-chlorocyclohexyl, 2-chlorocyclohexyl, 3-chlorocyclohexyl, 4-chlorocyclohexyl, 2,2-dichlorocyclohexyl, 3,3-dichlorocyclohexyl, 4,4-dichlorocyclohexyl, 3,3-dibromocyclohexyl, 4,4-dibromocyclohexyl, 3,3-diiodocyclohexyl, or 4,4-diiodocyclohexyl group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group” refers to a (C₁-C₆ haloalkyl)-(C₃-C₆ cyclo alkyl) group in which the haloalkyl moiety and the cycloalkyl moiety are as defined above, and examples of the “C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group” include a 2-trifluoromethylcyclopropyl, 2-trifluoromethylcyclobutyl, 3-trifluoromethylcyclobutyl, 2-trifluoromethylcyclopentyl, 3-trifluoromethylcyclopentyl, 2-trifluoromethylcyclohexyl, 3-trifluoromethylcyclohexyl, or 4-trifluoromethylcyclohexyl group.

In the present invention, unless otherwise specified, “C₃-C₆ cycloalkyl C₁-C₆ alkyl group” refers to a (C₃-C₆ cycloalkyl)-(C₁-C₆ alkyl) group in which the cycloalkyl moiety and the alkyl moiety are as defined above, and examples of the C₃-C₆ cycloalkyl C₁-C₆ alkyl group include a cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, 1-cyclopropylethyl, 2-cyclopropylethyl, 2-cyclobutylethyl, 2-cyclopentylethyl, or 2-cyclohexylethyl group.

In the present invention, unless otherwise specified, “C₃-C₆ halocycloalkyl C₁-C₆ alkyl group” refers to a (C₃-C₆ halocycloalkyl)-(C₁-C₆ alkyl)- group in which the halocycloalkyl moiety is as defined above, and examples of the “C₃-C₆ halocycloalkyl C₁-C₆ alkyl group” include a 2,2-difluorocyclopropylmethyl, 2,2-dichlorocyclopropylmethyl, 1-(2,2-difluorocyclopropyl)ethyl, 2-(2,2-difluorocyclopropyl)ethyl, 1-(2,2-dichlorocyclopropyl)ethyl, 2-(2,2-dichlorocyclopropyl)ethyl, 2-(2,2-difluorocyclopropyl)propyl, 3,3-difluorocyclobutylmethyl, 2,2,3,3-tetrafluorocyclobutylmethyl, 2-(2,2,3,3-tetrafluorocyclobutyl)ethyl, 2-(3,3-difluorocyclobutyl)ethyl, 2-(3,3-difluorocyclobutyl)propyl, 3,3-difluorocyclopentylmethyl or 2-(3,3-difluorocyclopentyl)propyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkylthio C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-S—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylthio C₁-C₆ alkyl group include a methylthiomethyl, ethylthiomethyl, n-propylthiomethyl, isopropylthiomethyl, 1-(methylthio)ethyl, 2-(methylthio)ethyl, 2-(ethylthio)ethyl, 1-(n-propylthio)ethyl, 2-(n-propylthio)ethyl, 1-(isopropylthio)ethyl, 2-(isopropylthio)ethyl, 1-(methylthio)propyl, 2-(methylthio)propyl, 3-(methylthio)propyl, 1-(ethylthio)propyl, 2-(ethylthio)propyl, 3-(ethylthio)propyl, 1-(n-propylthio)propyl, 2-(n-propylthio)propyl, 3-(n-propylthio)propyl, 1-(methylthio)butyl, 2-(methylthio)butyl, 3-(methylthio)butyl, 4-(methylthio)butyl, 1-(methylthio)pentyl, 2-(methylthio)pentyl, 3-(methylthio)pentyl, 4-(methylthio)pentyl, 5-(methylthio)pentyl, 2-(n-butylthio)ethyl, 2-(isobutylthio)ethyl, sec-butylthioethyl, 2-(tert-butylthio)ethyl, pentylthiomethyl, or hexylthiomethyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-S(═O)—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group include a methylsulfinylmethyl, ethylsulfinylmethyl, n-propylsulfinylmethyl, isopropylsulfinylmethyl, 1-(methylsulfinyl)ethyl, 2-(methylsulfinyl)ethyl, 2-(ethylsulfinyl)ethyl, 1-(n-propylsulfinyl)ethyl, 2-(n-propylsulfinyl)ethyl, 1-(isopropylsulfinyl)ethyl, 2-(isopropylsulfinyl)ethyl, 1-(methylsulfinyl)propyl, 2-(methylsulfinyl)propyl, 3-(methylsulfinyl)propyl, 1-(ethylsulfinyl)propyl, 2-(ethylsulfinyl)propyl, 3-(ethylsulfinyl)propyl, 1-(n-propylsulfinyl)propyl, 2-(n-propylsulfinyl)propyl, 3-(n-propylsulfinyl)propyl, 1-(methylsulfinyl)butyl, 2-(methylsulfinyl)butyl, 3-(methylsulfinyl)butyl, 4-(methylsulfinyl)butyl, 1-(methylsulfinyl)pentyl, 2-(methylsulfinyl)pentyl, 3-(methylsulfinyl)pentyl, 4-(methylsulfinyl)pentyl, 5-(methylsulfinyl)pentyl, 2-(n-butylsulfinyl)ethyl, 2-(isobutylsulfinyl)ethyl, sec-butylsulfinylethyl, 2-(tert-butylsulfinyl)ethyl, pentylsulfinylmethyl, or hexylsulfinylmethyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-S(═O)₂—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group include a methylsulfonylmethyl, ethylsulfonylmethyl, n-propylsulfonylmethyl, isopropylsulfonylmethyl, 1-(methylsulfonyl)ethyl, 2-(methylsulfonyl)ethyl, 2-(ethylsulfonyl)ethyl, 1-(n-propylsulfonyl)ethyl, 2-(n-propylsulfonyl)ethyl, 1-(isopropylsulfonyl)ethyl, 2-(isopropylsulfonyl)ethyl, 1-(methylsulfonyl)propyl, 2-(methylsulfonyl)propyl, 3-(methylsulfonyl)propyl, 1-(ethylsulfonyl)propyl, 2-(ethylsulfonyl)propyl, 3-(ethylsulfonyl)propyl, 1-(n-propylsulfonyl)propyl, 2-(n-propylsulfonyl)propyl, 3-(n-propylsulfonyl)propyl, 1-(methylsulfonyl)butyl, 2-(methylsulfonyl)butyl, 3-(methylsulfonyl)butyl, 4-(methylsulfonyl)butyl, 1-(methylsulfonyl)pentyl, 2-(methylsulfonyl)pentyl, 3-(methylsulfonyl)pentyl, 4-(methylsulfonyl)pentyl, 5-(methylsulfonyl)pentyl, 2-(n-butylsulfonyl)ethyl, 2-(isobutylsulfonyl)ethyl, sec-butylsulfonylethyl, 2-(tert-butylsulfonyl)ethyl, pentylsulfonylmethyl, or hexylsulfonylmethyl group.

In the present invention, “C₁-C₆ haloalkylthio C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-S—(C₁-C₆ alkyl)- group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylthio C₁-C₆ alkyl group include a 2-(difluoromethylthio)ethyl, 2-(trifluoromethylthio)ethyl, 2-(2,2-difluoroethylthio)ethyl, 2-(2,2,2-trifluoroethylthio)ethyl, 2-(3,3-difluoropropylthio)ethyl, 2-(3,3,3-trifluoroethylthio)ethyl, 3-(difluoromethylthio)propyl, 3-(trifluoromethylthio)propyl, 3-(2,2-difluoroethylthio)propyl, 3-(2,2,2-trifluoroethylthio)propyl, 3-(3,3-difluoropropylthio)propyl, 3-(3,3,3-trifluoropropylthio)propyl, 4-(trifluoromethylthio)butyl, or 5-(trifluoromethylthio)pentyl group.

In the present invention, “C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-S(═O)—(C₁-C₆ alkyl)- group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group include a 2-(difluoromethylsulfinyl)ethyl, 2-(trifluoromethylsulfinyl)ethyl, 2-(2,2-difluoroethylsulfinyl)ethyl, 2-(2,2,2-trifluoroethylsulfinyl)ethyl, 2-(3,3-difluoropropylsulfinyl)ethyl, 2-(3,3,3-trifluoroethylsulfinyl)ethyl, 3-(difluoromethylsulfinyl)propyl, 3-(trifluoromethylsulfinyl)propyl, 3-(2,2-difluoroethylsulfinyl)propyl, 3-(2,2,2-trifluoroethylsulfinyl)propyl, 3-(3,3-difluoropropylsulfinyl)propyl, 3-(3,3,3-trifluoropropylsulfinyl)propyl, 4-(trifluoromethylsulfinyl)butyl, or 5-(trifluoromethylsulfinyl)pentyl group.

In the present invention, “C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-S(═O)₂—(C₁-C₆ alkyl)- group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group include a 2-(difluoromethylsulfonyl)ethyl, 2-(trifluoromethylsulfonyl)ethyl, 2-(2,2-difluoroethylsulfonyl)ethyl, 2-(2,2,2-trifluoroethylsulfonyl)ethyl, 2-(3,3-difluoropropylsulfonyl)ethyl, 2-(3,3,3-trifluoroethylsulfonyl)ethyl, 3-(difluoromethylsulfonyl)propyl, 3-(trifluoromethylsulfonyl)propyl, 3-(2,2-difluoroethylsulfonyl)propyl, 3-(2,2,2-trifluoroethylsulfonyl)propyl, 3-(3,3-difluoropropylsulfonyl)propyl, 3-(3,3,3-trifluoropropylsulfonyl)propyl, 4-(trifluoromethylsulfonyl)butyl, or 5-(trifluoromethylsulfonyl)pentyl group.

In the present invention, “mono(C₁-C₆ alkyl)aminocarbonyl group” refers to a (C₁-C₆ alkyl)-NH—C(═O)— group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkyl)aminocarbonyl group include a methylaminocarbonyl, ethylaminocarbonyl, n-propylaminocarbonyl, isopropylaminocarbonyl, n-butylaminocarbonyl, isobutylaminocarbonyl, sec-butylaminocarbonyl, tert-butylaminocarbonyl, n-pentylaminocarbonyl, 1-methylbutylaminocarbonyl, 2-methylbutylaminocarbonyl, 3-methylbutylaminocarbonyl, 1-ethylpropylaminocarbonyl, 1,1-dimethylpropylaminocarbonyl, 1,2-dimethylpropylaminocarbonyl, 2,2-dimethylpropylaminocarbonyl, or n-hexylaminocarbonyl group.

In the present invention, “di(C₁-C₆ alkyl)aminocarbonyl group” refers to a (C₁-C₆ alkyl)₂N—C(═O)— group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C₁-C₆ alkyl)aminocarbonyl group include a dimethylaminocarbonyl, diethylaminocarbonyl, di(n-propyl)aminocarbonyl, diisopropylaminocarbonyl, dibutylaminocarbonyl, N-ethyl-N-methylaminocarbonyl, N-methyl-N-propylaminocarbonyl, N-isopropyl-N-methylaminocarbonyl, N-butyl-N-methylaminocarbonyl, N-(s-butyl)-N-methylaminocarbonyl, N-isobutyl-N-methylaminocarbonyl, N-pentyl-N-methylaminocarbonyl, N-ethyl-N-propylaminocarbonyl, N-ethyl-N-isopropylaminocarbonyl, or N-ethyl-N-butylaminocarbonyl group.

In the present invention, “mono(C₁-C₆ alkyl)aminothiocarbonyl group” refers to a (C₁-C₆ alkyl)-NH—C(═S)— group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkyl)aminothiocarbonyl group include a methylaminothiocarbonyl, ethylaminothiocarbonyl, n-propylaminothiocarbonyl, isopropylaminothiocarbonyl, n-butylaminothiocarbonyl, isobutylaminothiocarbonyl, sec-butylaminothiocarbonyl, tert-butylaminothiocarbonyl, n-pentylaminothiocarbonyl, 1-methylbutylaminothiocarbonyl, 2-methylbutylaminothiocarbonyl, 3-methylbutylaminothiocarbonyl, 1-ethylpropylaminothiocarbonyl, 1,1-dimethylpropylaminothiocarbonyl, 1,2-dimethylpropylaminothiocarbonyl, 2,2-dimethylpropylaminothiocarbonyl, or n-hexylaminothiocarbonyl group.

In the present invention, “di(C₁-C₆ alkyl)aminothiocarbonyl group” refers to a (C₁-C₆ alkyl)₂-N—C(═S)— group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C₁-C₆ alkyl)aminothiocarbonyl group include a dimethylaminothiocarbonyl, diethylaminothiocarbonyl, di(n-propyl)aminothiocarbonyl, diisopropylaminothiocarbonyl, dibutylaminothiocarbonyl, N-ethyl-N-methylaminothiocarbonyl, N-methyl-N-propylaminothiocarbonyl, N-isopropyl-N-methylaminothiocarbonyl, N-butyl-N-methylaminothiocarbonyl, N-(s-butyl)-N-methylaminothiocarbonyl, N-isobutyl-N-methylaminothiocarbonyl, N-pentyl-N-methylaminothiocarbonyl, N-ethyl-N-propylaminothiocarbonyl, N-ethyl-N-isopropylaminothiocarbonyl, or N-ethyl-N-butylaminothiocarbonyl group.

In the present invention, “C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-C(═O)—(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group include an acetonitrile, propionylmethyl, 2-methylpropionylmethyl, pivaloylmethyl, 2-acetylethyl, 2-propionylethyl, 2(2-methylpropionyl)ethyl, 2-pivaloylethyl, 3-acetylpropyl, 3-propionylpropyl, 3(2-methylpropionyl)propyl, or 3-pivaloylpropyl group.

In the present invention, “C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-C(═O)—(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group include a 2-oxo-3,3-difluoropropyl, 3-chloro-2-oxo-3,3-difluoropropyl, 2-oxo-3,3,3-trifluoropropyl, 3-oxo-4,4-difluorobutyl, 4-chloro-3-oxo-4,4-difluorobutyl, 3-oxo-4,4,4-trifluorobutyl, 3-oxo-4,4,5,5,5-pentafluoropentyl, 4-oxo-5,5,5-trifluoropentyl, or 4-oxo-5,5,6,6,6-pentafluorohexyl group.

In the present invention, “C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ alkoxy)-C(═O)—(C₁-C₆ alkyl)- group in which the alkoxy moiety is as defined above, and examples of the C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group include a methoxy carbonylmethyl, ethoxy carbonylmethyl, n-propoxy carbonylmethyl, isopropoxycarbonylmethyl, tert-butoxycarbonylmethyl, 1-(methoxycarbonyl)ethyl, 2-(methoxy carbonyl)ethyl, 1-(ethoxycarbonyl)ethyl, 2-(ethoxy carbonyl)ethyl, 1-(methoxy carbonyl)-1-methylethyl, 1-(ethoxy carbonyl)-1-methylethyl, or 2-(tert-butoxycarbonyl)ethyl group.

In the present invention, “aminocarbonyl C₁-C₆ alkyl group” refers to a H₂N—C(═O)—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the aminocarbonyl C₁-C₆ alkyl group include a carbamoylmethyl, 1-carbamoylethyl, or 2-carbamoylethyl group.

In the present invention, “mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-NH—C(═O)—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group include a N-methylcarbamoylmethyl, N-ethylcarbamoylmethyl, or N-(tert-butyl)carbamoylmethyl group.

In the present invention, “mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-NH—C(═O)—(C₁-C₆ alkyl)- group in which the haloalkyl moiety is as defined above, and examples of the mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group include a N-(2,2-difluoroethyl)carbamoylmethyl, N-(2,2,2-trifluoroethyl)carbamoylmethyl, 1-{N-(2,2-difluoroethyl)carbamoyl}ethyl, 1-{N-(2,2-trifluoroethyl)carbamoyl]}ethyl, 1-{N-(2,2-difluoroethyl)carbamoyl}-1-methylethyl, or 1-{N-(2,2-trifluoroethyl)carbamoyl}-1-methylethyl group.

In the present invention, “mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group” refers to a (C₃-C₆ cycloalkyl)-NH—C(═O)—(C₁-C₆ alkyl)- group in which the cycloalkyl moiety is as defined above, and examples of the mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group include a N-cyclopropylcarbamoylmethyl, N-cyclobutylcarbamoylmethyl, N-cyclopentylcarbamoylmethyl, or N-cyclohexylcarbamoylmethyl group.

In the present invention, “di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)₂-N—C(═O)—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group include a N,N-dimethylcarbamoylmethyl, N,N-diethylcarbamoylmethyl, N,N-dipropylcarbamoylmethyl, N-ethyl-N-methylcarbamoylmethyl, or N-methyl-N-propylcarbamoylmethyl group.

In the present invention, “mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-C(═O)—NH—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group include a 2-(acetylamino)ethyl, 2-(propanoylamino)ethyl, 2-(isopropanoylamino)ethyl, or 3-(acetylamino)propyl, 3-(acetylamino)butyl group.

In the present invention, “mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group” refers to a (C₁-C₆ alkoxy)-C(═O)—NH—(C₁-C₆ alkyl)- group in which the alkoxy moiety is as defined above, and examples of the mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group include a 2-(methoxycarbonylamino)ethyl, 2-(ethoxycarbonylamino)ethyl, or 2-(tert-butylcarbonylamino)ethyl group.

In the present invention, “mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-S(═O)₂—NH—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group include a 2-(methylsulfonylamino)ethyl, 2-(ethylsulfonylamino)ethyl, 2-(isopropylsulfonylamino)ethyl, 3-(methylsulfonylamino)propyl, or 4-(methylsulfonylamino)butyl group.

In the present invention, “mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-S(═O)₂—NH—(C₁-C₆ alkyl)- group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group include a 2-(difluoromethylsulfonylamino)ethyl, 2-(trifluoromethylsulfonylamino)ethyl, 3-(difluoromethylsulfonylamino)propyl, or 3-(trifluoromethylsulfonylamino)propyl group.

In the present invention, “mono(C₁-C₆ alkyl)aminosulfonyl group” refers to a (C₁-C₆ alkyl)-NH—S(═O)— group in which the alkyl moiety is as defined above, and examples of the mono(C₁-C₆ alkyl)aminosulfonyl group include a methylaminosulfonyl, ethylaminosulfonyl, n-propylaminosulfonyl, isopropylaminosulfonyl, n-butylaminosulfonyl, isobutylaminosulfonyl, sec-butylaminosulfonyl, tert-butylaminosulfonyl, n-pentylaminosulfonyl, 1-methylbutylaminosulfonyl, 2-methylbutylaminosulfonyl, 3-methylbutylaminosulfonyl, 1-ethylpropylaminosulfonyl, 1,1-dimethylpropylaminosulfonyl, 1,2-dimethylpropylaminosulfonyl, 2,2-dimethylpropylaminosulfonyl, or n-hexylaminosulfonyl group.

In the present invention, “di(C₁-C₆ alkyl)aminosulfonyl group” refers to a (C₁-C₆ alkyl)₂-N—S(═O)₂— group in which the alkyl moiety is as defined above, and the two alkyl groups may be different from each other, and examples of the di(C₁-C₆ alkyl)aminosulfonyl group include a dimethylaminosulfonyl, diethylaminosulfonyl, di(n-propyl)aminosulfonyl, diisopropylaminosulfonyl, dibutylaminosulfonyl, N-ethyl-N-methylaminosulfonyl, N-methyl-N-propylaminosulfonyl, N-isopropyl-N-methylaminosulfonyl, N-butyl-N-methylaminosulfonyl, N-(s-butyl)-N-methylaminosulfonyl, N-isobutyl-N-methylaminosulfonyl, N-pentyl-N-methylaminosulfonyl, N-ethyl-N-propylaminosulfocarbonyl, N-ethyl-N-isopropylaminosulfocarbonyl, or N-ethyl-N-butylaminosulfonyl group.

In the present invention, unless otherwise specified, “hydroxy C₁-C₆ alkyl group” refers to a (hydroxy)-(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the hydroxy C₁-C₆ alkyl group include a hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1-hydroxypropyl, 2-hydroxypropyl, 3-hydroxypropyl, 1-hydroxybutyl or 4-hydroxybutyl group.

In the present invention, unless otherwise specified, “hydroxyimino C₁-C₆ alkyl group” refers to a HO—N═(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the hydroxyimino C₁-C₆ alkyl group include a 1-(hydroxyimino)ethyl, 2-(hydroxyimino)ethyl, 1-(hydroxyimino)propyl, 2-(hydroxyimino)propyl, or 3-(hydroxyimino)propyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkoxyimino group” refers to a (C₁-C₆ alkyl)-O—N═C— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkoxyimino group include a methoxyimino, ethoxyimino, or isopropoxyimino group.

In the present invention, unless otherwise specified, “C₁-C₆ alkoxyimino C₁-C₆ alkyl group” refers to a (C₁-C₆ alkyl)-O—N═(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkoxyimino C₁-C₆ alkyl group include a 1-(methoxyimino)ethyl, 2-(methoxyimino)ethyl, 1-(methoxyimino)propyl, 2-(methoxyimino)propyl, 3-(methoxyimino)propyl, 1-(ethoxyimino)ethyl, 2-(ethoxyimino)ethyl, 1-(ethoxyimino)propyl, 2-(ethoxyimino)propyl, 3-(ethoxyimino)propyl, 1-(isopropoxyimino)ethyl, or 2-(isopropoxyimino)ethyl group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group” refers to a (C₁-C₆ haloalkyl)-O—N═(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group include a 2-(2,2-difluoroethoxyimino)ethyl, 2-(2,2,2-trifluoroethoxyimino)ethyl, 2-(2,2,2-trifluoroethoxyimino)propyl, or 3-(2,2,2-trifluoroethoxyimino)propyl group.

In the present invention, unless otherwise specified, examples of the “C₇-C₁₃ aralkyl group” include a benzyl, 1-phenylethyl, 2-phenylethyl, 2-phenylpropyl, (naphthalene-1-yl)methyl, or (naphthalene-2-yl)methyl group.

In the present invention, unless otherwise specified, “cyano C₁-C₆ alkyl group” refers to a (cyano)-(C₁-C₆ alkyl) group in which the alkyl moiety is as defined above, and examples of the cyano C₁-C₆ alkyl group include a cyanomethyl, 1-cyanoethyl, 2-cyanoethyl, 1-cyanopropyl, 3-cyanopropyl, 2-cyanopropane-2-yl, 1-cyanobutyl, 4-cyanobutyl, 5-cyanopentyl, or 6-cyanohexyl group.

In the present invention, unless otherwise specified, “cyano C₃-C₆ cycloalkyl group” refers to a (cyano)-(C₃-C₆ cycloalkyl) group in which the cycloalkyl moiety is as defined above, and examples of the cyano C₃-C₆ cycloalkyl group include a 1-cyanocyclopropyl, 2-cyanocyclopropyl, 1-cyanocyclobutyl, 3-cyanocyclobutyl, or 1-cyanocyclopentyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkylsulfonyloxy group” refers to a (C₁-C₆ alkyl)-S(═O)₂—O— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylsulfonyloxy group include a methylsulfonyloxy, ethylsulfonyloxy, or isopropylsulfonyloxy group.

In the present invention, unless otherwise specified, “C₁-C₆ alkylcarbonyl group” refers to a (C₁-C₆ alkyl)-C(═O)— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkylcarbonyl group include an acetyl, propionyl, 2-methylpropionyl, 2,2-dimethylpropionyl, butanoyl, 2-methylbutanoyl, 3-methylbutanoyl, 2-ethylbutanoyl, 2,2-dimethylbutanoyl, 2,3-dimethylbutanoyl, 3,3-dimethylbutanoyl, pentanoyl, 2-methylpentanoyl, 3-methylpentanoyl, 4-methylpentanoyl, or hexanoyl group.

In the present invention, unless otherwise specified, “C₁-C₆ alkoxy C₁-C₆ alkylcarbonyl group” refers to a (C₁-C₆ alkyl)-O—(C₁-C₆ alkyl)-C(═O)— group in which the alkyl moiety is as defined above, and examples of the C₁-C₆ alkoxy C₁-C₆ alkylcarbonyl group include a methoxyacetyl, ethoxyacetyl, propoxyacetyl, isopropoxyacetyl, butoxyacetyl, 2-methoxypropionyl, 3-methoxypropionyl, 2-ethoxypropionyl, 3-ethoxypropionyl, 2-methoxybutanoyl, 4-methoxybutanoyl, 2-methoxypentanoyl, or 5-methoxypentanoyl group.

In the present invention, unless otherwise specified, “C₃-C₆ cycloalkylcarbonyl group” refers to a (C₃-C₆ cycloalkyl)-C(═O)— group in which the cycloalkyl moiety is as defined above, and examples of the C₃-C₆ cycloalkylcarbonyl group include a cyclopropanecarbonyl, cyclobutanecarbonyl, cyclopentanecarbonyl, or cyclohexanecamyl group.

In the present invention, “C₁-C₆ alkoxycarbonyl group” refers to a (C₁-C₆ alkoxy)-C(═O)— group in which the alkoxy moiety is as defined above, and examples of the C₁-C₆ alkoxycarbonyl group include a methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl, n-butoxycarbonyl, isobutoxycarbonyl, sec-butoxycarbonyl, tert-butoxycarbonyl, n-pentoxycarbonyl, 1-methylbutoxycarbonyl, 2-methylbutoxy carbonyl, 3-methylbutoxy carbonyl, 1-ethylpropoxycarbonyl, 1,1-dimethylpropoxycarbonyl, 1,2-dimethylpropoxycarbonyl, or 2,2-dimethylpropoxycarbonyl group.

In the present invention, unless otherwise specified, “C₇-C₁₃ aralkylcarbonyl group” refers to a (C₇-C₁₃ aralkyl)-C(═O)— group in which the aralkyl moiety is as defined above, and examples of the C₇-C₁₃ aralkylcarbonyl group include a phenylethanoyl, 1-phenylpropanoyl, or 2-phenylpropanoyl group.

In the present invention, unless otherwise specified, “(C₁-C₆ alkyl)thiocarbonyl group” refers to a (C₁-C₆ alkyl)-C(═S)— group in which the alkyl moiety is as defined above, and examples of the (C₁-C₆ alkyl)thiocarbonyl group include a methylthiocarbonyl, ethylthiocarbonyl, n-propopylthiocarbonyl, isopropylthiocarbonyl, n-butylthiocarbonyl, isobutylthiocarbonyl, sec-butylthiocarbonyl, tert-butylthiocarbonyl, or n-pentylthiocarbonyl group.

In the present invention, unless otherwise specified, “(C₁-C₆ alkoxy)thiocarbonyl group” refers to a (C₁-C₆ alkyl)-O—C(═S)— group in which the alkyl moiety is as defined above, and examples of the (C₁-C₆ alkoxy)thiocarbonyl group include a methoxythiocarbonyl, ethoxythiocarbonyl, n-propoxythiocarbonyl, isopropoxythiocarbonyl, n-butoxythiocarbonyl, isobutoxythiocarbonyl, sec-butoxythiocarbonyl, tert-butoxythiocarbonyl, n-pentoxythiocarbonyl, 1-methyl butoxythiocarbonyl, 2-methyl butoxythiocarbonyl, 3-methyl butoxythiocarbonyl, 1-ethylpropoxythiocarbonyl, 1,1-dimethylpropoxythiocarbonyl, 1,2-dimethylpropoxythiocarbonyl, or 2,2-dimethylpropoxythiocarbonyl group.

In the present invention, “C₃-C₆ cycloalkyl C₁-C₆ alkylcarbonyl group” refers to a (C₃-C₆ cycloalkyl C₁-C₆ alkyl)-C(═O)— group in which the cycloalkyl alkyl moiety is as defined above, and examples of the C₃-C₆ cycloalkyl C₁-C₆ alkylcarbonyl group include a 2-cyclopropylacetyl, 2-cyclobutylacetyl, 2-cyclopentylacetyl, 2-cyclohexylacetyl, 2-cyclopropylpropanoyl, or 2-cyclopropylbutanoyl group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkylthio group” refers to a (C₁-C₆ haloalkyl)-S— group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylthio group include a fluoromethylthio, difluoromethylthio, trifluoromethylthio, trichloromethylthio, 2,2,2-trifluoroethylthio, pentafluoroethylthio, 2,2,2-trichloroethylthio, 3,3,3-trifluoropropylthio, 1,1,2,3,3,3-hexafluoropropyl, heptafluoropropylthio, 1,1,1,3,3,3-hexafluoropropane-2-ylthio, heptafluoropropane-2-ylthio, or 4,4,4-trifluorobutylthio group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkylsulfinyl group” refers to a (C₁-C₆ haloalkyl)-S(═O)— group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylsulfinyl group include a difluoromethylsulfinyl, trifluoromethylsulfinyl, trichloromethylsulfinyl, 2,2,2-trifluoroethylsulfinyl, 2,2,2-trichloroethylsulfinyl, pentafluoroethylsulfinyl, 3,3,3-trifluoropropylsulfinyl, heptafluoropropylsulfinyl, or heptafluoro-2-propylsulfinyl group.

In the present invention, unless otherwise specified, “C₁-C₆ haloalkylsulfonyl group” refers to a (C₁-C₆ haloalkyl)-S(═O)₂— group in which the haloalkyl moiety is as defined above, and examples of the C₁-C₆ haloalkylsulfonyl group include a difluoromethylsulfonyl, trifluoromethylsulfonyl, trichloromethylsulfonyl, 2,2,2-trifluoroethylsulfonyl, pentafluoroethylsulfonyl, 3,3,3-trifluoropropylsulfonyl, heptafluoropropylsulfonyl, or heptafluoro-2-propylsulfonyl group.

In the present invention, the wording “agriculturally acceptable salt” refers to a salt of a hydroxyl group, a carboxyl group, an amino group or the like when such a group exists in the structure of the present compound represented by general formula [I] or [II], or a nitrogen atom in a pyridine ring, with metal or an organic base, or a salt with a mineral acid or an organic acid, and examples of the metal include alkali metal such as sodium or potassium, and alkali earth metal such as magnesium or calcium, examples of the organic base include triethylamine or diisopropylamine, examples of the mineral acid include phosphoric acid, hydrochloric acid, hydrobromic acid, hydroiodic acid, boric acid, or sulfuric acid, and examples of the organic acid include formic acid, acetic acid, lactic acid, ascorbic acid, succinic acid, fumaric acid, maleic acid, oxalic acid, citric acid, benzoic acid, salicylic acid, tartaric acid, methanesulfonic acid, 4-toluenesulfonic acid, or trifluoromethanesulfonic acid.

Next, representative compound examples of compounds included in the pyrazole-3-carboxylic acid amide derivative of the present invention represented by general formula [I] are shown in Table 1 to Table 93, and representative compound examples of compounds included in the pyrazole-3-carboxylic acid derivative of the present invention represented by general formula [II] are shown in Table 94 to Table 149. However, the compounds included in the derivatives of the present invention are not limited to these. The compound numbers in Tables are referred to in the following description.

The compounds included in the pyrazole-3-carboxylic acid amide derivative or pyrazole-3-carboxylic acid derivative of the present invention can have geometrical isomers of E-body and Z-body depending on the kind of the substituent, and the present invention encompasses such E-body, Z-body, or a mixture containing E-body and Z-body in any ratio. The compounds encompassed in the present invention can have optical isomers caused by the existence of one or two or more asymmetric carbon atoms and asymmetric sulfur atoms, and the present invention encompasses any optically active substances, racemic bodies, or diastereomers.

In the present specification, the following signs in tables respectively represent the corresponding groups as shown below.

CF₃: trifluoromethyl

(4-CF₃)Ph: 4-trifluoromethylphenyl

(2-F-4-CF₃)Ph: 2-fluoro-4-trifluoromethylphenyl

TABLE 1

Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0001 H H H H H H H H O 0 A-0002 H H H H H CH₃ H H O 0 A-0003 H H H H H CH₂CH₃ H H O 0 A-0004 H H H H H CH(CH₃)₂ H H O 0 A-0005 H H H H H C(CH₃)₃ H H O 0 A-0006 H H H H H CH₂CH₂CH₃ H H O 0 A-0007 H H H H H CH₂CH(CH₃)₂ H H O 0 A-0008 H H H H H CH(CH₃)CH₂CH₃ H H O 0 A-0009 H H H H H CH(CH₂CH₃)CH₂CH₃ H H O 0 A-0010 H H H H H CH₂C(CH₃)₃ H H O 0 A-0011 H H H H H CH₂(CH₂)₂CH₃ H H O 0 A-0012 H H H H H CH₂CH₂CH(CH₃)₂ H H O 0 A-0013 H H H H H CH₂CH(CH₃)CH₂CH₃ H H O 0 A-0014 H H H H H CH(CH₃)CH₂CH₂CH₃ H H O 0 A-0015 H H H H H CH₂CH(CH₂CH₃)CH₂CH₃ H H O 0 A-0016 H H H H H CH(CH₂CH₃)CH₂CH₂CH₃ H H O 0 A-0017 H H H H H CH₂CH₂C(CH₃)₃ H H O 0 A-0018 H H H H H CH₂(CH₂)₃CH₃ H H O 0 A-0019 H H H H H CH₂CH₂CH₂CH(CH₃)₂ H H O 0 A-0020 H H H H H CH₂(CH₂)₄CH₃ H H O 0 A-0021 H H H H H CH₂CH₂CH₂CH₂CH(CH₃)₂ H H O 0 A-0022 H H H H H CH₂(CH₂)₅CH₃ H H O 0 A-0023 H H H H H CH₂(CH₂)₆CH₃ H H O 0 A-0024 H H H H H CH₂OCH₃ H H O 0 A-0025 H H H H H CH₂OCH₂CH₃ H H O 0 A-0026 H H H H H CH₂CH₂OCH₃ H H O 0 A-0027 H H H H H CH₂CH₂OCH₂CH₃ H H O 0 A-0028 H H H H H CH₂CH₂CH₂OCH₃ H H O 0 A-0029 H H H H H CH₂CH₂CH₂OCH₂CH₃ H H O 0 A-0030 H H H H H CF₃ H H O 0 A-0031 H H H H H CHF₂ H H O 0 A-0032 H H H H H CH₂CF₃ H H O 0 A-0033 H H H H H CH₂CHF₂ H H O 0 A-0034 H H H H H CH₂CClF₂ H H O 0 A-0035 H H H H H CF₂CHCl₂ H H O 0 A-0036 H H H H H CF₂CCl₃ H H O 0 A-0037 H H H H H CH₂CH₂Cl H H O 0 A-0038 H H H H H CHClCHCl₂ H H O 0 A-0039 H H H H H CH₂CCl₃ H H O 0 A-0040 H H H H H CH₂CBrF₂ H H O 0 A-0041 H H H H H CF₂CF₃ H H O 0 A-0042 H H H H H CF₂CHF₂ H H O 0 A-0043 H H H H H CH₂CH₂CF₃ H H O 0 A-0044 H H H H H CH₂CF₂CF₃ H H O 0 A-0045 H H H H H CH₂CF₂CHF₂ H H O 0 A-0046 H H H H H CF₂CHFCF₃ H H O 0 A-0047 H H H H H CF₂CF₂CF₃ H H O 0 A-0048 H H H H H CH₂CH₂CH₂Cl H H O 0 A-0049 H H H H H CH₂CHClCH₂Cl H H O 0 A-0050 H H H H H CH₂CF₂CF₂CF₃ H H O 0 A-0051 H H H H H CH₂CF₂CHFCF₃ H H O 0 A-0052 H H H H H CH₂CH₂CH₂CF₃ H H O 0 A-0053 H H H H H CH₂CH₂CF₂CF₃ H H O 0 A-0054 H H H H H CF₂CF₂CF₂CF₃ H H O 0 A-0055 H H H H H CH₂CH₂CH(CF₃)₂ H H O 0 A-0056 H H H H H CH₂CH₂CH(CH₃)CF₃ H H O 0

TABLE 2 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0057 H H H H H CF₂CF₂CF₂CF₂CF₃ H H O 0 A-0058 H H H H H CH₂CF₂CF₂CF₂CF₃ H H O 0 A-0059 H H H H H CH₂CH₂CH₂CH₂CF₃ H H O 0 A-0060 H H H H H CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-0061 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-0062 H H H H H CH₂CF₂CF₂CF₂CF₂CF₃ H H O 0 A-0063 H H H H H CH₂CH₂CH₂CH₂CH₂CF₃ H H O 0 A-0064 H H H H H CH₂CF₂CF₂CF₂CF₂CHF₂ H H O 0 A-0065 H H H H H CH₂CF₂CF₂CF₂CF₂CF₂CF₃ H H O 0 A-0066 H H H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H H O 0 A-0067 H H H H H CH₂CF₂CF₂CF₂CF₂CF₂CHF₂ H H O 0 A-0068 H H H H H CF₂CHFOCH₃ H H O 0 A-0069 H H H H H CF₂CHFOCH₂CH₃ H H O 0 A-0070 H H H H H CH₂CH₂OCH₂CF₃ H H O 0 A-0071 H H H H H CF₂CHFOCF₃ H H O 0 A-0072 H H H H H CF₂CHFOCF₂CF₃ H H O 0 A-0073 H H H H H CF₂CHFOCF₂CF₂CF₃ H H O 0 A-0074 H H H H H CH₂CH═CH₂ H H O 0 A-0075 H H H H H CH₂CH═CHCl H H O 0 A-0076 H H H H H CH₂CH═CCl₂ H H O 0 A-0077 H H H H H CH₂CH═C(CH₃)CF₃ H H O 0 A-0078 H H H H H CH₂CH₂CF═CF₂ H H O 0 A-0079 H H H H H CH₂CH₂CH═CF₂ H H O 0 A-0080 H H H H H CH₂C≡CH H H O 0 A-0081 H H H H H CH₂C≡CCH₃ H H O 0 A-0082 H H H H H CH₂C≡CC(CH₃)₃ H H O 0 A-0083 H H H H H CH₂C≡C(cyclopropyl) H H O 0 A-0084 H H H H H CH₂C≡CI H H O 0 A-0085 H H H H H CH₂C≡CCF₃ H H O 0 A-0086 H H H H H cyclopropyl H H O 0 A-0087 H H H H H cyclobutyl H H O 0 A-0088 H H H H H cyclopentyl H H O 0 A-0089 H H H H H cyclohexyl H H O 0 A-0090 H H H H H 4,4-difluorocyclohexyl H H O 0 A-0091 H H H H H 4-trifluoromethylcyclohexyl H H O 0 A-0092 H H H H H CH₂(cyclopropyl) H H O 0 A-0093 H H H H H CH₂(cyclobutyl) H H O 0 A-0094 H H H H H CH₂(cyclopentyl) H H O 0 A-0095 H H H H H CH₂(cyclohexyl) H H O 0 A-0096 H H H H H CH₂CH₂(cyclopropyl) H H O 0 A-0097 H H H H H CH₂(2,2-difluorocyclopropyl) H H O 0 A-0098 H H H H H CH₂(2,2-dichlorocyclopropyl) H H O 0 A-0099 H H H H H CH₂(4,4-difluorocyclohexyl) H H O 0 A-0100 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-0101 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-0102 H H H H H CH₂CH₂(4,4-difluorocyclohexyl) H H O 0 A-0103 H H H H H CH₂SCH₃ H H O 0 A-0104 H H H H H CH₂SCH₂CH₃ H H O 0 A-0105 H H H H H CH₂CH₂SCH₃ H H O 0 A-0106 H H H H H CH₂CH₂SCH₂CH₃ H H O 0 A-0107 H H H H H CH₂CH₂CH₂SCH₃ H H O 0 A-0108 H H H H H CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-0109 H H H H H CH(CH₃)SCH₃ H H O 0 A-0110 H H H H H CH(CH₃)SCH₂CH₃ H H O 0 A-0111 H H H H H CH₂CH(CH₃)SCH₃ H H O 0 A-0112 H H H H H CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-0113 H H H H H CH₂CH₂SCH(CH₃)₂ H H O 0 A-0114 H H H H H CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-0115 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-0116 H H H H H CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-0117 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0

TABLE 3 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0118 H H H H H CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-0119 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-0120 H H H H H CH₂CH₂CH₂CH₂SCH₃ H H O 0 A-0121 H H H H H CH₂CH₂CH₂CH₂CH₂SCH₃ H H O 0 A-0122 H H H H H CH₂SOCH₃ H H O 0 A-0123 H H H H H CH₂CH₂SOCH₃ H H O 0 A-0124 H H H H H CH₂CH₂SOCH₂CH₃ H H O 0 A-0125 H H H H H CH₂CH₂SOCH(CH₃)₂ H H O 0 A-0126 H H H H H CH₂CH₂CH₂SOCH₃ H H O 0 A-0127 H H H H H CH(CH₃)SOCH₃ H H O 0 A-0128 H H H H H CH₂CH(CH₃)SOCH₃ H H O 0 A-0129 H H H H H CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-0130 H H H H H CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-0131 H H H H H CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-0132 H H H H H CH₂CH₂CH₂CH₂SOCH₃ H H O 0 A-0133 H H H H H CH₂CH₂CH₂CH₂CH₂SOCH₃ H H O 0 A-0134 H H H H H CH₂SO₂CH₃ H H O 0 A-0135 H H H H H CH₂CH₂SO₂CH₃ H H O 0 A-0136 H H H H H CH₂CH₂SO₂CH₂CH₃ H H O 0 A-0137 H H H H H CH₂CH₂SO₂CH(CH₃)₂ H H O 0 A-0138 H H H H H CH₂CH₂CH₂SO₂CH₃ H H O 0 A-0139 H H H H H CH(CH₃)SO₂CH₃ H H O 0 A-0140 H H H H H CH₂CH(CH₃)SO₂CH₃ H H O 0 A-0141 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-0142 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-0143 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-0144 H H H H H CH₂CH₂CH₂CH₂SO₂CH₃ H H O 0 A-0145 H H H H H CH₂CH₂CH₂CH₂CH₂SO₂CH₃ H H O 0 A-0146 H H H H H CH₂SCF₃ H H O 0 A-0147 H H H H H CH₂SCHF₂ H H O 0 A-0148 H H H H H CH₂SCH₂CF₃ H H O 0 A-0149 H H H H H CH₂SCH₂CHF₂ H H O 0 A-0150 H H H H H CH₂SCF₂CF₃ H H O 0 A-0151 H H H H H CH₂CH₂SCF₃ H H O 0 A-0152 H H H H H CH₂CH₂SCH₂CF₃ H H O 0 A-0153 H H H H H CH₂CH₂CH₂SCF₃ H H O 0 A-0154 H H H H H CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-0155 H H H H H CH(CH₃)SCF₃ H H O 0 A-0156 H H H H H CH(CH₃)SCH₂CF₃ H H O 0 A-0157 H H H H H CH₂CH(CH₃)SCF₃ H H O 0 A-0158 H H H H H CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-0159 H H H H H CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-0160 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-0161 H H H H H CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-0162 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-0163 H H H H H CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-0164 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-0165 H H H H H CH₂CH₂CH₂CH₂SCF₃ H H O 0 A-0166 H H H H H CH₂CH₂CH₂CH₂CH₂SCF₃ H H O 0 A-0167 H H H H H CH₂SOCF₃ H H O 0 A-0168 H H H H H CH₂CH₂SOCF₃ H H O 0 A-0169 H H H H H CH₂CH₂CH₂SOCF₃ H H O 0 A-0170 H H H H H CH(CH₃)SOCF₃ H H O 0 A-0171 H H H H H CH₂CH(CH₃)SOCF₃ H H O 0 A-0172 H H H H H CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-0173 H H H H H CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-0174 H H H H H CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-0175 H H H H H CH₂SO₂CF₃ H H O 0 A-0176 H H H H H CH₂CH₂SO₂CF₃ H H O 0 A-0177 H H H H H CH₂CH₂SO₂CH₂CF₃ H H O 0 A-0178 H H H H H CH₂CH₂CH₂SO₂CF₃ H H O 0

TABLE 4 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0179 H H H H H CH(CH₃)SO₂CF₃ H H O 0 A-0180 H H H H H CH₂CH(CH₃)SO₂CF₃ H H O 0 A-0181 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-0182 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-0183 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0 A-0184 H H H H H CH₂C(═O)CH₃ H H O 0 A-0185 H H H H H CH₂C(═O)CH₂CH₃ H H O 0 A-0186 H H H H H CH₂C(═O)C(CH₃)₃ H H O 0 A-0187 H H H H H CH₂CH₂C(═O)CH₃ H H O 0 A-0188 H H H H H CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-0189 H H H H H CH₂C(═O)CF₃ H H O 0 A-0190 H H H H H CH₂CH₂C(═O)CF₃ H H O 0 A-0191 H H H H H CH₂C(═O)OCH₃ H H O 0 A-0192 H H H H H CH₂C(═O)OCH₂CH₃ H H O 0 A-0193 H H H H H CH₂C(═O)OC(CH₃)₃ H H O 0 A-0194 H H H H H CH₂CH₂C(═O)OCH₃ H H O 0 A-0195 H H H H H CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-0196 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-0197 H H H H H CH₂C(═O)NH₂ H H O 0 A-0198 H H H H H CH₂CH₂C(═O)NH₂ H H O 0 A-0199 H H H H H CH₂C(═O)NHCH₃ H H O 0 A-0200 H H H H H CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-0201 H H H H H CH₂CH₂C(═O)NHCH₃ H H O 0 A-0202 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-0203 H H H H H CH₂C(═O)NH(cyclopropyl) H H O 0 A-0204 H H H H H CH₂C(═O)NHCH₂CHF₂ H H O 0 A-0205 H H H H H CH₂C(═O)NHCH₂CF₃ H H O 0 A-0206 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-0207 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-0208 H H H H H CH(CH₃)C(═O)NHCH₂CHF₂ H H O 0 A-0209 H H H H H CH(CH₃)C(═O)NHCH₂CF₃ H H O 0 A-0210 H H H H H C(CH₃)₂C(═O)NHCH₂CHF₂ H H O 0 A-0211 H H H H H C(CH₃)₂C(═O)NHCH₂CF₃ H H O 0 A-0212 H H H H H CH₂C(═O)N(CH₃)₂ H H O 0 A-0213 H H H H H CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-0214 H H H H H CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-0215 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-0216 H H H H H CH₂CH₂NHC(═O)OCH₃ H H O 0 A-0217 H H H H H CH₂CH₂NHC(═O)OC(CH₃)₃ H H O 0 A-0218 H H H H H CH₂CH₂CH₂NHC(═O)OCH₃ H H O 0 A-0219 H H H H H CH₂CH₂CH₂NHC(═O)OC(CH₃)₃ H H O 0 A-0220 H H H H H CH₂CH₂NHSO₂CHF₂ H H O 0 A-0221 H H H H H CH₂CH₂NHSO₂CF₃ H H O 0 A-0222 H H H H H CH₂CH₂CH₂NHSO₂CHF₂ H H O 0 A-0223 H H H H H CH₂CH₂CH₂NHSO₂CF₃ H H O 0 A-0224 H H H H H CH₂CH₂OH H H O 0 A-0225 H H H H H CH₂CH(OH)CH₃ H H O 0 A-0226 H H H H H CH₂CH₂CH₂OH H H O 0 A-0227 H H H H H CH₂CH(OH)CH₂CH₃ H H O 0 A-0228 H H H H H CH₂CH(OH)C(CH₃)₃ H H O 0 A-0229 H H H H H CH₂CH₂CH(OH)CH₃ H H O 0 A-0230 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-0231 H H H H H CH₂C(═NOH)CH₃ H H O 0 A-0232 H H H H H CH₂C(═NOH)CH₂CH₃ H H O 0 A-0233 H H H H H CH₂C(═NOH)C(CH₃)₃ H H O 0 A-0234 H H H H H CH₂C(═NOCH₃)CH₃ H H O 0 A-0235 H H H H H CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-0236 H H H H H CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-0237 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-0238 H H H H H CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-0239 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0

TABLE 5 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0240 H H H H H CH₂Ph H H O 0 A-0241 H H H H H CH₂(2-F)Ph H H O 0 A-0242 H H H H H CH₂(3-F)Ph H H O 0 A-0243 H H H H H CH₂(4-F)Ph H H O 0 A-0244 H H H H H CH₂(2-Cl)Ph H H O 0 A-0245 H H H H H CH₂(3-Cl)Ph H H O 0 A-0246 H H H H H CH₂(4-Cl)Ph H H O 0 A-0247 H H H H H CH₂(2-CF₃)Ph H H O 0 A-0248 H H H H H CH₂(3-CF₃)Ph H H O 0 A-0249 H H H H H CH₂(4-CF₃)Ph H H O 0 A-0250 H H H H H CH₂(2-F—4-CF₃)Ph H H O 0 A-0251 H H H H H CH₂(naphthalen-1-yl) H H O 0 A-0252 H H H H H CH₂(naphthalen-2-yl) H H O 0 A-0253 H H H H H CH(CH₃)Ph H H O 0 A-0254 H H H H H CH₂CH₂Ph H H O 0 A-0255 H H H H H H CH₃ H O 0 A-0256 H H H H H CH₃ CH₃ H O 0 A-0257 H H H H H CH₂CH₃ CH₃ H O 0 A-0258 H H H H H CH(CH₃)2 CH₃ H O 0 A-0259 H H H H H CH₂CH(CH₃)₂ CH₃ H O 0 A-0260 H H H H H CH(CH₃)CH₂CH₃ CH₃ H O 0 A-0261 H H H H H CH₂C(CH₃)₃ CH₃ H O 0 A-0262 H H H H H CH₂(CH₂)₂CH₃ CH₃ H O 0 A-0263 H H H H H CH₂(CH₂)₃CH₃ CH₃ H O 0 A-0264 H H H H H CH₂(CH₂)₄CH₃ CH₃ H O 0 A-0265 H H H H H CH₂(CH₂)₆CH₃ CH₃ H O 0 A-0266 H H H H H CH₂OCH₃ CH₃ H O 0 A-0267 H H H H H CH₂OCH₂CH₃ CH₃ H O 0 A-0268 H H H H H CH₂CH₂OCH₃ CH₃ H O 0 A-0269 H H H H H CH₂CH₂OCH₂CH₃ CH₃ H O 0 A-0270 H H H H H CF₃ CH₃ H O 0 A-0271 H H H H H CHF₂ CH₃ H O 0 A-0272 H H H H H CH₂CF₃ CH₃ H O 0 A-0273 H H H H H CH₂CHF₂ CH₃ H O 0 A-0274 H H H H H CH₂CClF₂ CH₃ H O 0 A-0275 H H H H H CH₂CBrF₂ CH₃ H O 0 A-0276 H H H H H CF₂CF₃ CH₃ H O 0 A-0277 H H H H H CF₂CHF₂ CH₃ H O 0 A-0278 H H H H H CH₂CH₂CF₃ CH₃ H O 0 A-0279 H H H H H CH₂CF₂CF₃ CH₃ H O 0 A-0280 H H H H H CH₂CF₂CHF₂ CH₃ H O 0 A-0281 H H H H H CF₂CHFCF₃ CH₃ H O 0 A-0282 H H H H H CF₂CF₂CF₃ CH₃ H O 0 A-0283 H H H H H CH₂CF₂CF₂CF₂ CH₃ H O 0 A-0284 H H H H H CH₂CF₂CHFCF₃ CH₃ H O 0 A-0285 H H H H H CH₂CH₂CH₂CF₃ CH₃ H O 0 A-0286 H H H H H CH₂CH₂CF₂CF₃ CH₃ H O 0 A-0287 H H H H H CF₂CF₂CF₂CF₃ CH₃ H O 0 A-0288 H H H H H CH₂CH₂CH(CF₃)₂ CH₃ H O 0 A-0289 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₃ H O 0 A-0290 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₃ H O 0 A-0291 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₃ H O 0 A-0292 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₃ H O 0 A-0293 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₃ H O 0 A-0294 H H H H H CH₂CH═CH₂ CH₃ H O 0 A-0295 H H H H H CH₂CH═CHCl CH₃ H O 0 A-0296 H H H H H CH₂CH═CCl₂ CH₃ H O 0 A-0297 H H H H H CH₂CH₂CF═CF₂ CH₃ H O 0 A-0298 H H H H H CH₂CH₂CH═CF₂ CH₃ H O 0 A-0299 H H H H H CH₂C≡CH CH₃ H O 0 A-0300 H H H H H CH₂C≡CCH₃ CH₃ H O 0

TABLE 6 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0301 H H H H H CH₂C≡CI CH₃ H O 0 A-0302 H H H H H CH₂C≡CCF₃ CH₃ H O 0 A-0303 H H H H H cyclobutyl CH₃ H O 0 A-0304 H H H H H cyclopentyl CH₃ H O 0 A-0305 H H H H H cyclohexyl CH₃ H O 0 A-0306 H H H H H 4,4-difluorocyclohexyl CH₃ H O 0 A-0307 H H H H H CH₂(cyclopropyl) CH₃ H O 0 A-0308 H H H H H CH₂(cyclobutyl) CH₃ H O 0 A-0309 H H H H H CH₂(cyclopentyl) CH₃ H O 0 A-0310 H H H H H CH₂CH₂(cyclopropyl) CH₃ H O 0 A-0311 H H H H H CH₂(2,2-difluorocyclopropyl) CH₃ H O 0 A-0312 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₃ H O 0 A-0313 H H H H H CH₂(4,4-difluorocyclohexyl) CH₃ H O 0 A-0314 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₃ H O 0 A-0315 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₃ H O 0 A-0316 H H H H H CH₂SCH₃ CH₃ H O 0 A-0317 H H H H H CH₂SCH₂CH₃ CH₃ H O 0 A-0318 H H H H H CH₂CH₂SCH₃ CH₃ H O 0 A-0319 H H H H H CH₂CH₂SCH₂CH₃ CH₃ H O 0 A-0320 H H H H H CH₂CH₂CH₂SCH₃ CH₃ H O 0 A-0321 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₃ H O 0 A-0322 H H H H H CH(CH₃)SCH₃ CH₃ H O 0 A-0323 H H H H H CH(CH₃)SCH₂CH₃ CH₃ H O 0 A-0324 H H H H H CH₂CH(CH₃)SCH₃ CH₃ H O 0 A-0325 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₃ H O 0 A-0326 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₃ H O 0 A-0327 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₃ H O 0 A-0328 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₃ H O 0 A-0329 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₃ H O 0 A-0330 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₃ H O 0 A-0331 H H H H H CH₂CH₂CH(CH₃)SCH₃CH₃ CH₃ H O 0 A-0332 H H H H H CH₂SOCH₃ CH₃ H O 0 A-0333 H H H H H CH₂CH₂SOCH₃ CH₃ H O 0 A-0334 H H H H H CH₂CH₂CH₂SOCH₃ CH₃ H O 0 A-0335 H H H H H CH(CH₃)SOCH₃ CH₃ H O 0 A-0336 H H H H H CH₂CH(CH₃)SOCH₃ CH₃ H O 0 A-0337 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₃ H O 0 A-0338 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₃ H O 0 A-0339 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₃ H O 0 A-0340 H H H H H CH₂SO2CH₃ CH₃ H O 0 A-0341 H H H H H CH₂CH₂SO2CH₃ CH₃ H O 0 A-0342 H H H H H CH₂CH₂CH₂SO2CH₃ CH₃ H O 0 A-0343 H H H H H CH(CH₃)SO2CH₃ CH₃ H O 0 A-0344 H H H H H CH₂CH(CH₃)SO2CH₃ CH₃ H O 0 A-0345 H H H H H CH(CH₃)CH₂CH₂SO2CH₃ CH₃ H O 0 A-0346 H H H H H CH₂CH(CH₃)CH₂SO2CH₃ CH₃ H O 0 A-0347 H H H H H CH₂CH₂CH(CH₃)SO2CH₃ CH₃ H O 0 A-0348 H H H H H CH₂SCF₃ CH₃ H O 0 A-0349 H H H H H CH₂SCHF₂ CH₃ H O 0 A-0350 H H H H H CH₂SCH₂CF₃ CH₃ H O 0 A-0351 H H H H H CH₂SCH₂CHF₂ CH₃ H O 0 A-0352 H H H H H CH₂SCF₂CF₃ CH₃ H O 0 A-0353 H H H H H CH₂CH₂SCF₃ CH₃ H O 0 A-0354 H H H H H CH₂CH₂SCH₂CF₃ CH₃ H O 0 A-0355 H H H H H CH₂CH₂CH₂SCF₃ CH₃ H O 0 A-0356 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₃ H O 0 A-0357 H H H H H CH(CH₃)SCF₃ CH₃ H O 0 A-0358 H H H H H CH(CH₃)SCH₂CF₃ CH₃ H O 0 A-0359 H H H H H CH₂CH(CH₃)SCF₃ CH₃ H O 0 A-0360 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₃ H O 0 A-0361 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₃ H O 0

TABLE 7 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0362 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₃ H O 0 A-0363 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₃ H O 0 A-0364 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₃ H O 0 A-0365 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₃ H O 0 A-0366 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₃ H O 0 A-0367 H H H H H CH₂SOCF₃ CH₃ H O 0 A-0368 H H H H H CH₂CH₂SOCF₃ CH₃ H O 0 A-0369 H H H H H CH₂CH₂CH₂SOCF₃ CH₃ H O 0 A-0370 H H H H H CH(CH₃)SOCF₃ CH₃ H O 0 A-0371 H H H H H CH₂CH(CH₃)SOCF₃ CH₃ H O 0 A-0372 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₃ H O 0 A-0373 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₃ H O 0 A-0374 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₃ H O 0 A-0375 H H H H H CH₂SO₂CF₃ CH₃ H O 0 A-0376 H H H H H CH₂CH₂SO₂CF₃ CH₃ H O 0 A-0377 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₃ H O 0 A-0378 H H H H H CH(CH₃)SO₂CF₃ CH₃ H O 0 A-0379 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₃ H O 0 A-0380 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₃ H O 0 A-0381 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₃ H O 0 A-0382 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₃ H O 0 A-0383 H H H H H CH₂C(═O)CH₃ CH₃ H O 0 A-0384 H H H H H CH₂C(═O)CH₂CH₃ CH₃ H O 0 A-0385 H H H H H CH₂C(═O)C(CH₃)₃ CH₃ H O 0 A-0386 H H H H H CH₂CH₂C(═O)CH₃ CH₃ H O 0 A-0387 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₃ H O 0 A-0388 H H H H H CH₂C(═O)CF₃ CH₃ H O 0 A-0389 H H H H H CH₂CH₂C(═O)CF₃ CH₃ H O 0 A-0390 H H H H H CH₂C(═O)OCH₃ CH₃ H O 0 A-0391 H H H H H CH₂C(═O)OCH₂CH₃ CH₃ H O 0 A-0392 H H H H H CH₂C(═O)OC(CH₃)₃ CH₃ H O 0 A-0393 H H H H H CH₂CH₂C(═O)OCH₃ CH₃ H O 0 A-0394 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₃ H O 0 A-0395 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₃ H O 0 A-0396 H H H H H CH₂C(═O)NH₂ CH₃ H O 0 A-0397 H H H H H CH₂CH₂C(═O)NH₂ CH₃ H O 0 A-0398 H H H H H CH₂C(═O)NHCH₃ CH₃ H O 0 A-0399 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₃ H O 0 A-0400 H H H H H CH₂CH₂C(═O)NHCH₃ CH₃ H O 0 A-0401 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₃ H O 0 A-0402 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₃ H O 0 A-0403 H H H H H CH₂C(═O)NHCH₂CF₃ CH₃ H O 0 A-0404 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₃ H O 0 A-0405 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₃ H O 0 A-0406 H H H H H CH₂C(═O)N(CH₃)₂ CH₃ H O 0 A-0407 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₃ H O 0 A-0408 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₃ H O 0 A-0409 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₃ H O 0 A-0410 H H H H H CH₂CH₂OH CH₃ H O 0 A-0411 H H H H H CH₂CH(OH)CH₃ CH₃ H O 0 A-0412 H H H H H CH₂CH₂CH₂OH CH₃ H O 0 A-0413 H H H H H CH₂CH(OH)CH₂CH₃ CH₃ H O 0 A-0414 H H H H H CH₂CH(OH)C(CH₃)₃ CH₃ H O 0 A-0415 H H H H H CH₂CH₂CH(OH)CH₃ CH₃ H O 0 A-0416 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₃ H O 0 A-0417 H H H H H CH₂C(═NOH)CH₃ CH₃ H O 0 A-0418 H H H H H CH₂C(═NOH)CH₂CH₃ CH₃ H O 0 A-0419 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₃ H O 0 A-0420 H H H H H CH₂C(═NOCH₃)CH₃ CH₃ H O 0 A-0421 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₃ H O 0 A-0422 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₃ H O 0

TABLE 8 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0423 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₃ H O 0 A-0424 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₃ H O 0 A-0425 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₃ H O 0 A-0426 H H H H H CH₂Ph CH₃ H O 0 A-0427 H H H H H CH₂(2-F)Ph CH₃ H O 0 A-0428 H H H H H CH₂(3-F)Ph CH₃ H O 0 A-0429 H H H H H CH₂(4-F)Ph CH₃ H O 0 A-0430 H H H H H CH₂(2-Cl)Ph CH₃ H O 0 A-0431 H H H H H CH₂(3-Cl)Ph CH₃ H O 0 A-0432 H H H H H CH₂(4-Cl)Ph CH₃ H O 0 A-0433 H H H H H CH₂(2-CF₃)Ph CH₃ H O 0 A-0434 H H H H H CH₂(3-CF₃)Ph CH₃ H O 0 A-0435 H H H H H CH₂(4-CF₃)Ph CH₃ H O 0 A-0436 H H H H H CH₂(naphthalen-1-yl) CH₃ H O 0 A-0437 H H H H H CH₂(naphthalen-2-yl) CH₃ H O 0 A-0438 H H H H H CH₂CH₂Ph CH₃ H O 0 A-0439 H H H H H H CH₂CH₃ H O 0 A-0440 H H H H H CH₃ CH₂CH₃ H O 0 A-0441 H H H H H CH₂CH₃ CH₂CH₃ H O 0 A-0442 H H H H H CH(CH₃)₂ CH₂CH₃ H O 0 A-0443 H H H H H CH₂CH₂CH₃ CH₂CH₃ H O 0 A-0444 H H H H H CH₂CH(CH₃)₂ CH₂CH₃ H O 0 A-0445 H H H H H CH(CH₃)CH₂CH₃ CH₂CH₃ H O 0 A-0446 H H H H H CH₂C(CH₃)₃ CH₂CH₃ H O 0 A-0447 H H H H H CH₂(CH₂)₂CH₃ CH₂CH₃ H O 0 A-0448 H H H H H CH₂(CH₂)₃CH₃ CH₂CH₃ H O 0 A-0449 H H H H H CH₂(CH₂)₄CH₃ CH₂CH₃ H O 0 A-0450 H H H H H CH₂(CH₂)₆CH₃ CH₂CH₃ H O 0 A-0451 H H H H H CH₂OCH₃ CH₂CH₃ H O 0 A-0452 H H H H H CH₂OCH₂CH₃ CH₂CH₃ H O 0 A-0453 H H H H H CH₂CH₂OCH₃ CH₂CH₃ H O 0 A-0454 H H H H H CH₂CH₂OCH₂CH₃ CH₂CH₃ H O 0 A-0455 H H H H H CF₃ CH₂CH₃ H O 0 A-0456 H H H H H CHF₂ CH₂CH₃ H O 0 A-0457 H H H H H CH₂CF₃ CH₂CH₃ H O 0 A-0458 H H H H H CH₂CHF₂ CH₂CH₃ H O 0 A-0459 H H H H H CH₂CClF₂ CH₂CH₃ H O 0 A-0460 H H H H H CH₂CBrF₂ CH₂CH₃ H O 0 A-0461 H H H H H CF₂CF₃ CH₂CH₃ H O 0 A-0462 H H H H H CF₂CHF₂ CH₂CH₃ H O 0 A-0463 H H H H H CH₂CH₂CF₃ CH₂CH₃ H O 0 A-0464 H H H H H CH₂CF₂CF₃ CH₂CH₃ H O 0 A-0465 H H H H H CH₂CF₂CHF₂ CH₂CH₃ H O 0 A-0466 H H H H H CF₂CHFCF₃ CH₂CH₃ H O 0 A-0467 H H H H H CF₂CF₂CF₃ CH₂CH₃ H O 0 A-0468 H H H H H CH₂CF₂CF₂CF₃ CH₂CH₃ H O 0 A-0469 H H H H H CH₂CF₂CHFCF₃ CH₂CH₃ H O 0 A-0470 H H H H H CH₂CH₂CH₂CF₃ CH₂CH₃ H O 0 A-0471 H H H H H CH₂CH₂CF₂CF₃ CH₂CH₃ H O 0 A-0472 H H H H H CF₂CF₂CF₂CF₃ CH₂CH₃ H O 0 A-0473 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CH₃ H O 0 A-0474 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ H O 0 A-0475 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ H O 0 A-0476 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ H O 0 A-0477 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ H O 0 A-0478 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ H O 0 A-0479 H H H H H CF₂CHFOCH₃ CH₂CH₃ H O 0 A-0480 H H H H H CF₂CHFOCH₂CH₃ CH₂CH₃ H O 0 A-0481 H H H H H CH₂CH₂OCH₂CF₃ CH₂CH₃ H O 0 A-0482 H H H H H CF₂CHFOCF₃ CH₂CH₃ H O 0 A-0483 H H H H H CF₂CHFOCF₂CF₃ CH₂CH₃ H O 0

TABLE 9 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0484 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ H O 0 A-0485 H H H H H CH₂CH═CH₂ CH₂CH₃ H O 0 A-0486 H H H H H CH₂CH═CHCl CH₂CH₃ H O 0 A-0487 H H H H H CH₂CH═CCl₂ CH₂CH₃ H O 0 A-0488 H H H H H CH₂CH₂CF═CF₂ CH₂CH₃ H O 0 A-0489 H H H H H CH₂CH₂CH═CF₂ CH₂CH₃ H O 0 A-0490 H H H H H CH₂C≡CH CH₂CH₃ H O 0 A-0491 H H H H H CH₂C≡CCH₃ CH₂CH₃ H O 0 A-0492 H H H H H CH₂C≡CI CH₂CH₃ H O 0 A-0493 H H H H H CH₂C≡CCF₃ CH₂CH₃ H O 0 A-0494 H H H H H cyclobutyl CH₂CH₃ H O 0 A-0495 H H H H H cyclopentyl CH₂CH₃ H O 0 A-0496 H H H H H cyclohexyl CH₂CH₃ H O 0 A-0497 H H H H H 4,4-difluorocyclohexyl CH₂CH₃ H O 0 A-0498 H H H H H CH₂(cyclopropyl) CH₂CH₃ H O 0 A-0499 H H H H H CH₂(cyclobutyl) CH₂CH₃ H O 0 A-0500 H H H H H CH₂(cyclopentyl) CH₂CH₃ H O 0 A-0501 H H H H H CH₂CH₂(cyclopropyl) CH₂CH₃ H O 0 A-0502 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ H O 0 A-0503 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ H O 0 A-0504 H H H H H CH₂(4,4-difluorocyclohexyl) CH₂CH₃ H O 0 A-0505 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ H O 0 A-0506 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ H O 0 A-0507 H H H H H CH₂SCH₃ CH₂CH₃ H O 0 A-0508 H H H H H CH₂SCH₂CH₃ CH₂CH₃ H O 0 A-0509 H H H H H CH₂CH₂SCH₃ CH₂CH₃ H O 0 A-0510 H H H H H CH₂CH₂SCH₂CH₃ CH₂CH₃ H O 0 A-0511 H H H H H CH₂CH₂CH₂SCH₃ CH₂CH₃ H O 0 A-0512 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ H O 0 A-0513 H H H H H CH(CH₃)SCH₃ CH₂CH₃ H O 0 A-0514 H H H H H CH(CH₃)SCH₂CH₃ CH₂CH₃ H O 0 A-0515 H H H H H CH₂CH(CH₃)SCH₃ CH₂CH₃ H O 0 A-0516 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ H O 0 A-0517 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ H O 0 A-0518 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ H O 0 A-0519 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ H O 0 A-0520 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ H O 0 A-0521 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ H O 0 A-0522 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ H O 0 A-0523 H H H H H CH₂SOCH₃ CH₂CH₃ H O 0 A-0524 H H H H H CH₂CH₂SOCH₃ CH₂CH₃ H O 0 A-0525 H H H H H CH₂CH₂CH₂SOCH₃ CH₂CH₃ H O 0 A-0526 H H H H H CH(CH₃)SOCH₃ CH₂CH₃ H O 0 A-0527 H H H H H CH₂CH(CH₃)SOCH₃ CH₂CH₃ H O 0 A-0528 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ H O 0 A-0529 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ H O 0 A-0530 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ H O 0 A-0531 H H H H H CH₂SO₂CH₃ CH₂CH₃ H O 0 A-0532 H H H H H CH₂CH₂SO₂CH₃ CH₂CH₃ H O 0 A-0533 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ H O 0 A-0534 H H H H H CH(CH₃)SO₂CH₃ CH₂CH₃ H O 0 A-0535 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ H O 0 A-0536 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ H O 0 A-0537 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ H O 0 A-0538 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ H O 0 A-0539 H H H H H CH₂SCF₃ CH₂CH₃ H O 0 A-0540 H H H H H CH₂SCHF₂ CH₂CH₃ H O 0 A-0541 H H H H H CH₂SCH₂CF₃ CH₂CH₃ H O 0 A-0542 H H H H H CH₂SCH₂CHF₂ CH₂CH₃ H O 0 A-0543 H H H H H CH₂SCF₂CF₃ CH₂CH₃ H O 0 A-0544 H H H H H CH₂CH₂SCF₃ CH₂CH₃ H O 0

TABLE 10 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0545 H H H H H CH₂CH₂SCH₂CF₃ CH₂CH₃ H O 0 A-0546 H H H H H CH₂CH₂CH₂SCF₃ CH₂CH₃ H O 0 A-0547 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ H O 0 A-0548 H H H H H CH(CH₃)SCF₃ CH₂CH₃ H O 0 A-0549 H H H H H CH(CH₃)SCH₂CF₃ CH₂CH₃ H O 0 A-0550 H H H H H CH₂CH(CH₃)SCF₃ CH₂CH₃ H O 0 A-0551 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ H O 0 A-0552 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ H O 0 A-0553 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ H O 0 A-0554 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ H O 0 A-0555 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ H O 0 A-0556 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ H O 0 A-0557 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ H O 0 A-0558 H H H H H CH₂SOCF₃ CH₂CH₃ H O 0 A-0559 H H H H H CH₂CH₂SOCF₃ CH₂CH₃ H O 0 A-0560 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CH₃ H O 0 A-0561 H H H H H CH(CH₃)SOCF₃ CH₂CH₃ H O 0 A-0562 H H H H H CH₂CH(CH₃)SOCF₃ CH₂CH₃ H O 0 A-0563 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ H O 0 A-0564 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ H O 0 A-0565 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ H O 0 A-0566 H H H H H CH₂SO₂CF₃ CH₂CH₃ H O 0 A-0567 H H H H H CH₂CH₂SO₂CF₃ CH₂CH₃ H O 0 A-0568 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ H O 0 A-0569 H H H H H CH(CH₃)SO₂CF₃ CH₂CH₃ H O 0 A-0570 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ H O 0 A-0571 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ H O 0 A-0572 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ H O 0 A-0573 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ H O 0 A-0574 H H H H H CH₂C(═O)CH₃ CH₂CH₃ H O 0 A-0575 H H H H H CH₂C(═O)CH₂CH₃ CH₂CH₃ H O 0 A-0576 H H H H H CH₂C(═O)C(CH₃)₃ CH₂CH₃ H O 0 A-0577 H H H H H CH₂CH₂C(═O)CH₃ CH₂CH₃ H O 0 A-0578 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ H O 0 A-0579 H H H H H CH₂C(═O)CF₃ CH₂CH₃ H O 0 A-0580 H H H H H CH₂CH₂C(═O)CF₃ CH₂CH₃ H O 0 A-0581 H H H H H CH₂C(═O)OCH₃ CH₂CH₃ H O 0 A-0582 H H H H H CH₂C(═O)OCH₂CH₃ CH₂CH₃ H O 0 A-0583 H H H H H CH₂C(═O)OC(CH₃)₃ CH₂CH₃ H O 0 A-0584 H H H H H CH₂CH₂C(═O)OCH₃ CH₂CH₃ H O 0 A-0585 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ H O 0 A-0586 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ H O 0 A-0587 H H H H H CH₂C(═O)NH₂ CH₂CH₃ H O 0 A-0588 H H H H H CH₂CH₂C(═O)NH₂ CH₂CH₃ H O 0 A-0589 H H H H H CH₂C(═O)NHCH₃ CH₂CH₃ H O 0 A-0590 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ H O 0 A-0591 H H H H H CH₂CH₂C(═O)NHCH₃ CH₂CH₃ H O 0 A-0592 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ H O 0 A-0593 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ H O 0 A-0594 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ H O 0 A-0595 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ H O 0 A-0596 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ H O 0 A-0597 H H H H H CH₂C(═O)N(CH₃)₂ CH₂CH₃ H O 0 A-0598 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ H O 0 A-0599 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ H O 0 A-0600 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ H O 0 A-0601 H H H H H CH₂CH₂OH CH₂CH₃ H O 0 A-0602 H H H H H CH₂CH(OH)CH₃ CH₂CH₃ H O 0 A-0603 H H H H H CH₂CH₂CH₂OH CH₂CH₃ H O 0 A-0604 H H H H H CH₂CH(OH)CH₂CH₃ CH₂CH₃ H O 0 A-0605 H H H H H CH₂CH(OH)C(CH₃)₃ CH₂CH₃ H O 0

TABLE 11 Compund R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0606 H H H H H CH₂CH₂CH(OH)CH₃ CH₂CH₃ H O 0 A-0607 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ H O 0 A-0608 H H H H H CH₂C(═NOH)CH₃ CH₂CH₃ H O 0 A-0609 H H H H H CH₂C(═NOH)CH₂CH₃ CH₂CH₃ H O 0 A-0610 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ H O 0 A-0611 H H H H H CH₂C(═NOCH₃)CH₃ CH₂CH₃ H O 0 A-0612 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ H O 0 A-0613 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ H O 0 A-0614 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ H O 0 A-0615 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ H O 0 A-0616 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ H O 0 A-0617 H H H H H CH₂Ph CH₂CH₃ H O 0 A-0618 H H H H H CH₂(2-F)Ph CH₂CH₃ H O 0 A-0619 H H H H H CH₂(3-F)Ph CH₂CH₃ H O 0 A-0620 H H H H H CH₂(4-F)Ph CH₂CH₃ H O 0 A-0621 H H H H H CH₂(2-Cl)Ph CH₂CH₃ H O 0 A-0622 H H H H H CH₂(3-Cl)Ph CH₂CH₃ H O 0 A-0623 H H H H H CH₂(4-Cl)Ph CH₂CH₃ H O 0 A-0624 H H H H H CH₂(2-CF₃)Ph CH₂CH₃ H O 0 A-0625 H H H H H CH₂(3-CF₃)Ph CH₂CH₃ H O 0 A-0626 H H H H H CH₂(4-CF₃)Ph CH₂CH₃ H O 0 A-0627 H H H H H CH₂(naphthalen-1-yl) CH₂CH₃ H O 0 A-0628 H H H H H CH₂(naphthalen-2-yl) CH₂CH₃ H O 0 A-0629 H H H H H CH₂CH₂Ph CH₂CH₃ H O 0 A-0630 H H H H H H CH(CH₃)₂ H O 0 A-0631 H H H H H CH₃ CH(CH₃)₂ H O 0 A-0632 H H H H H CH₂CH₃ CH(CH₃)₂ H O 0 A-0633 H H H H H CH(CH₃)₂ CH(CH₃)₃ H O 0 A-0634 H H H H H CH₂CH₂CH₃ CH(CH₃)₂ H O 0 A-0635 H H H H H CH₂CH(CH₃)₂ CH(CH₃)₂ H O 0 A-0636 H H H H H CH(CH₃)CH₃CH₃ CH(CH₃)₂ H O 0 A-0637 H H H H H CH₂C(CH₃)3 CH(CH₃)₂ H O 0 A-0638 H H H H H CH₂(CH₂)₂CH₃ CH(CH₃)₂ H O 0 A-0639 H H H H H CH₂(CH₂)₃CH₃ CH(CH₃)₂ H O 0 A-0640 H H H H H CH₂(CH₂)₄CH₃ CH(CH₃)₂ H O 0 A-0641 H H H H H CH₂OCH₃ CH(CH₃)₂ H O 0 A-0642 H H H H H CH₂OCH₂CH₃ CH(CH₃)₂ H O 0 A-0643 H H H H H CH₂CH₂OCH₃ CH(CH₃)₂ H O 0 A-0644 H H H H H CH₂CH₂OCH₂CH₃ CH(CH₃)₂ H O 0 A-0645 H H H H H CF₃ CH(CH₃)₂ H O 0 A-0646 H H H H H CHF₂ CH(CH₃)₂ H O 0 A-0647 H H H H H CH₂CF₃ CH(CH₃)₂ H O 0 A-0648 H H H H H CH₂CHF₂ CH(CH₃)₂ H O 0 A-0649 H H H H H CH₂CClF₂ CH(CH₃)₂ H O 0 A-0650 H H H H H CH₂CBrF₂ CH(CH₃)₂ H O 0 A-0651 H H H H H CF₂CF₃ CH(CH₃)₂ H O 0 A-0652 H H H H H CF₂CHF₂ CH(CH₃)₂ H O 0 A-0653 H H H H H CH₂CH₂CF₃ CH(CH₃)₂ H O 0 A-0654 H H H H H CH₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0655 H H H H H CH₂CF₂CHF₂ CH(CH₃)₂ H O 0 A-0656 H H H H H CF₂CHFCF₃ CH(CH₃)₂ H O 0 A-0657 H H H H H CF₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0658 H H H H H CH₂CF₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0659 H H H H H CH₂CF₂CHFCF₃ CH(CH₃)₂ H O 0 A-0660 H H H H H CH₂CH₂CH₂CF₃ CH(CH₃)₂ H O 0 A-0661 H H H H H CH₂CH₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0662 H H H H H CF₂CF₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0663 H H H H H CH₂CH₂CH(CF₃)2 CH(CH₃)₂ H O 0 A-0664 H H H H H CF₂CF₂CF₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0665 H H H H H CH₂CF₂CF₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0666 H H H H H CH₂CH₂CH₂CH₂CF₃ CH(CH₃)₂ H O 0

TABLE 12 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0667 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH(CH₃)₂ H O 0 A-0668 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH(CH₃)₂ H O 0 A-0669 H H H H H CF₂CHFOCH₃ CH(CH₃)₂ H O 0 A-0670 H H H H H CF₂CHFOCH₂CH₃ CH(CH₃)₂ H O 0 A-0671 H H H H H CH₂CH₂OCH₂CF₃ CH(CH₃)₂ H O 0 A-0672 H H H H H CF₂CHFOCF₃ CH(CH₃)₂ H O 0 A-0673 H H H H H CF₂CHFOCF₂CF₃ CH(CH₃)₂ H O 0 A-0674 H H H H H CF₂CHFOCF₂CF₂CF₃ CH(CH₃)₂ H O 0 A-0675 H H H H H CH₂CH═CH₂ CH(CH₃)₂ H O 0 A-0676 H H H H H CH₂CH═CHCl CH(CH₃)₂ H O 0 A-0677 H H H H H CH₂CH═CCl₂ CH(CH₃)₂ H O 0 A-0678 H H H H H CH₂CH₂CF═CF₂ CH(CH₃)₂ H O 0 A-0679 H H H H H CH₂CH₂CH═CF₂ CH(CH₃)₂ H O 0 A-0680 H H H H H CH₂C≡CH CH(CH₃)₂ H O 0 A-0681 H H H H H CH₂C≡CCH₃ CH(CH₃)₂ H O 0 A-0682 H H H H H CH₂C≡CI CH(CH₃)₂ H O 0 A-0683 H H H H H CH₂C≡CCF₃ CH(CH₃)₂ H O 0 A-0684 H H H H H cydobutyl CH(CH₃)₂ H O 0 A-0685 H H H H H cyclopentyl CH(CH₃)₂ H O 0 A-0686 H H H H H cyclohexyl CH(CH₃)₂ H O 0 A-0687 H H H H H 4,4-difluorocyclohexyl CH(CH₃)₂ H O 0 A-0688 H H H H H CH₂(cyclopropyl) CH(CH₃)₂ H O 0 A-0689 H H H H H CH₂(cyclobutyl) CH(CH₃)₂ H O 0 A-0690 H H H H H CH₂(cyclopentyl) CH(CH₃)₂ H O 0 A-0691 H H H H H CH₂CH₂(cyclopropyl) CH(CH₃)₂ H O 0 A-0692 H H H H H CH₂(2,2-difluorocyclopropyl) CH(CH₃)₂ H O 0 A-0693 H H H H H CH₂(2,2-dichlorocyclopropyl) CH(CH₃)₂ H O 0 A-0694 H H H H H CH₂(4,4-difluorocyclohexyl) CH(CH₃)₂ H O 0 A-0695 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH(CH₃)₂ H O 0 A-0696 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH(CH₃)₂ H O 0 A-0697 H H H H H CH₂SCH₃ CH(CH₃)₂ H O 0 A-0698 H H H H H CH₂SCH₂CH₃ CH(CH₃)₂ H O 0 A-0699 H H H H H CH₂CH₂SCH₃ CH(CH₃)₂ H O 0 A-0700 H H H H H CH₂CH₂SCH₂CH₃ CH(CH₃)₂ H O 0 A-0701 H H H H H CH₂CH₂CH₂SCH₃ CH(CH₃)₂ H O 0 A-0702 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH(CH₃)₂ H O 0 A-0703 H H H H H CH(CH₃)SCH₃ CH(CH₃)₂ H O 0 A-0704 H H H H H CH(CH₃)SCH₂CH₃ CH(CH₃)₂ H O 0 A-0705 H H H H H CH₂CH(CH₃)SCH₃ CH(CH₃)₂ H O 0 A-0706 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH(CH₃)₂ H O 0 A-0707 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH(CH₃)₂ H O 0 A-0708 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH(CH₃)₂ H O 0 A-0709 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH(CH₃)₂ H O 0 A-0710 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH(CH₃)₂ H O 0 A-0711 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH(CH₃)₂ H O 0 A-0712 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH(CH₃)₂ H O 0 A-0713 H H H H H CH₂SOCH₃ CH(CH₃)₂ H O 0 A-0714 H H H H H CH₂CH₂SOCH₃ CH(CH₃)₂ H O 0 A-0715 H H H H H CH₂CH₂CH₂SOCH₃ CH(CH₃)₂ H O 0 A-0716 H H H H H CH(CH₃)SOCH₃ CH(CH₃)₂ H O 0 A-0717 H H H H H CH₂CH(CH₃)SOCH₃ CH(CH₃)₂ H O 0 A-0718 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH(CH₃)₂ H O 0 A-0719 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH(CH₃)₂ H O 0 A-0720 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH(CH₃)₂ H O 0 A-0721 H H H H H CH₂SO2CH₃ CH(CH₃)₂ H O 0 A-0722 H H H H H CH₂CH₂SO2CH₃ CH(CH₃)₂ H O 0 A-0723 H H H H H CH₂CH₂CH₂SO2CH₃ CH(CH₃)₂ H O 0 A-0724 H H H H H CH(CH₃)SO2CH₃ CH(CH₃)₂ H O 0 A-0725 H H H H H CH₂CH(CH₃)SO2CH₃ CH(CH₃)₂ H O 0 A-0726 H H H H H CH(CH₃)CH₂CH₂SO2CH₃ CH(CH₃)₂ H O 0 A-0727 H H H H H CH₂CH(CH₃)CH₂SO2CH₃ CH(CH₃)₂ H O 0

TABLE 13 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0728 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH(CH₃)₂ H O 0 A-0729 H H H H H CH₂SOF₃ CH(CH₃)₂ H O 0 A-0730 H H H H H CH₂SCHF₂ CH(CH₃)₂ H O 0 A-0731 H H H H H CH₂SCH₂CF₃ CH(CH₃)₂ H O 0 A-0732 H H H H H CH₂SCH₂CHF₂ CH(CH₃)₂ H O 0 A-0733 H H H H H CH₂SCF₂CF₃ CH(CH₃)₂ H O 0 A-0734 H H H H H CH₂CH₂SCF₃ CH(CH₃)₂ H O 0 A-0735 H H H H H CH₂CH₂SCH₂CF₃ CH(CH₃)₂ H O 0 A-0736 H H H H H CH₂CH₂CH₂SCF₃ CH(CH₃)₂ H O 0 A-0737 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH(CH₃)₂ H O 0 A-0738 H H H H H CH(CH₃)SCF₃ CH(CH₃)₂ H O 0 A-0739 H H H H H CH(CH₃)SCH₂CF₃ CH(CH₃)₂ H O 0 A-0740 H H H H H CH₂CH(CH₃)SCF₃ CH(CH₃)₂ H O 0 A-0741 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH(CH₃)₂ H O 0 A-0742 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH(CH₃)₂ H O 0 A-0743 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH(CH₃)₂ H O 0 A-0744 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH(CH₃)₂ H O 0 A-0745 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH(CH₃)₂ H O 0 A-0746 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH(CH₃)₂ H O 0 A-0747 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH(CH₃)₂ H O 0 A-0748 H H H H H CH₂SOCF₃ CH(CH₃)₂ H O 0 A-0749 H H H H H CH₂CH₂SOCF₃ CH(CH₃)₂ H O 0 A-0750 H H H H H CH₂CH₂CH₂SOCF₃ CH(CH₃)₂ H O 0 A-0751 H H H H H CH(CH₃)SOCF₃ CH(CH₃)₂ H O 0 A-0752 H H H H H CH₂CH(CH₃)SOCF₃ CH(CH₃)₂ H O 0 A-0753 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH(CH₃)₂ H O 0 A-0754 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH(CH₃)₂ H O 0 A-0755 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH(CH₃)₂ H O 0 A-0756 H H H H H CH₂SO₂CF₃ CH(CH₃)₂ H O 0 A-0757 H H H H H CH₂CH₂SO₂CF₃ CH(CH₃)₂ H O 0 A-0758 H H H H H CH₂CH₂CH₂SO₂CF₃ CH(CH₃)₂ H O 0 A-0759 H H H H H CH(CH₃)SO₂CF₃ CH(CH₃)₂ H O 0 A-0760 H H H H H CH₂CH(CH₃)SO₂CF₃ CH(CH₃)₂ H O 0 A-0761 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH(CH₃)₂ H O 0 A-0762 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH(CH₃)₂ H O 0 A-0763 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH(CH₃)₂ H O 0 A-0764 H H H H H CH₂C(═O)CH₃ CH(CH₃)₂ H O 0 A-0765 H H H H H CH₂C(═O)CH₂CH₃ CH(CH₃)₂ H O 0 A-0766 H H H H H CH₂C(═O)C(CH₃)₃ CH(CH₃)₂ H O 0 A-0767 H H H H H CH₂CH₂C(═O)CH₃ CH(CH₃)₂ H O 0 A-0768 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH(CH₃)₂ H O 0 A-0769 H H H H H CH₂C(═O)CF₃ CH(CH₃)₂ H O 0 A-0770 H H H H H CH₂CH₂C(═O)CF₃ CH(CH₃)₂ H O 0 A-0771 H H H H H CH₂C(═O)OCH₃ CH(CH₃)₂ H O 0 A-0772 H H H H H CH₂C(═O)OCH₂CH₃ CH(CH₃)₂ H O 0 A-0773 H H H H H CH₂C(═O)OC(CH₃)₃ CH(CH₃)₂ H O 0 A-0774 H H H H H CH₂CH₂C(═O)OCH₃ CH(CH₃)₂ H O 0 A-0775 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH(CH₃)₂ H O 0 A-0776 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH(CH₃)₂ H O 0 A-0777 H H H H H CH₂C(═O)NH₂ CH(CH₃)₂ H O 0 A-0778 H H H H H CH₂CH₂C(═O)NH₂ CH(CH₃)₂ H O 0 A-0779 H H H H H CH₂C(═O)NHCH₃ CH(CH₃)₂ H O 0 A-0780 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH(CH₃)₂ H O 0 A-0781 H H H H H CH₂CH₂C(═O)NHCH₃ CH(CH₃)₂ H O 0 A-0782 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH(CH₃)₂ H O 0 A-0783 H H H H H CH₂C(═O)NHCH₂CHF₂ CH(CH₃)₂ H O 0 A-0784 H H H H H CH₂C(═O)NHCH₂CF₃ CH(CH₃)₂ H O 0 A-0785 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH(CH₃)₂ H O 0 A-0786 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH(CH₃)₂ H O 0 A-0787 H H H H H CH₂C(═O)N(CH₃)₂ CH(CH₃)₂ H O 0 A-0788 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH(CH₃)₂ H O 0

TABLE 14 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0789 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH(CH₃)₂ H O 0 A-0790 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH(CH₃)₂ H O 0 A-0791 H H H H H CH₂CH₂OH CH(CH₃)₂ H O 0 A-0792 H H H H H CH₂CH(OH)CH₃ CH(CH₃)₂ H O 0 A-0793 H H H H H CH₂CH₂CH₂OH CH(CH₃)₂ H O 0 A-0794 H H H H H CH₂CH(OH)CH₂CH₃ CH(CH₃)₂ H O 0 A-0795 H H H H H CH₂CH(OH)C(CH₃)₃ CH(CH₃)₂ H O 0 A-0796 H H H H H CH₂CH₂CH(OH)CH₃ CH(CH₃)₂ H O 0 A-0797 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH(CH₃)₂ H O 0 A-0798 H H H H H CH₂C(═NOH)CH₃ CH(CH₃)₂ H O 0 A-0799 H H H H H CH₂C(═NOH)CH₂CH₃ CH(CH₃)₂ H O 0 A-0800 H H H H H CH₂C(═NOH)C(CH₃)₃ CH(CH₃)₂ H O 0 A-0801 H H H H H CH₂C(═NOCH₃)CH₃ CH(CH₃)₂ H O 0 A-0802 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH(CH₃)₂ H O 0 A-0803 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH(CH₃)₂ H O 0 A-0804 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH(CH₃)₂ H O 0 A-0805 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH(CH₃)₂ H O 0 A-0806 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH(CH₃)₂ H O 0 A-0807 H H H H H CH₂Ph CH(CH₃)₂ H O 0 A-0808 H H H H H CH₂(2-F)Ph CH(CH₃)₂ H O 0 A-0809 H H H H H CH₂(3-F)Ph CH(CH₃)₂ H O 0 A-0810 H H H H H CH₂(4-F)Ph CH(CH₃)₂ H O 0 A-0811 H H H H H CH₂(2-Cl)Ph CH(CH₃)₂ H O 0 A-0812 H H H H H CH₂(3-Cl)Ph CH(CH₃)₂ H O 0 A-0813 H H H H H CH₂(4-Cl)Ph CH(CH₃)₂ H O 0 A-0814 H H H H H CH₂(2-CF₃)Ph CH(CH₃)₂ H O 0 A-0815 H H H H H CH₂(3-CF₃)Ph CH(CH₃)₂ H O 0 A-0816 H H H H H CH₂(4-CF₃)Ph CH(CH₃)₂ H O 0 A-0817 H H H H H CF₂(naphthalen-1-yl) CH(CH₃)₂ H O 0 A-0818 H H H H H CH₂(naphthalen-2-yl) CH(CH₃)₂ H O 0 A-0819 H H H H H CH₂CH₂Ph CH(CH₃)₂ H O 0 A-0820 H H H H H H CH₂CH₂CH₃ H O 0 A-0821 H H H H H CH₃ CH₂CH₂CH₃ H O 0 A-0822 H H H H H CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0823 H H H H H CH(CH₃)₂ CH₂CH₂CH₃ H O 0 A-0824 H H H H H CH₂CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0825 H H H H H CH₂CH(CH₃)₂ CH₂CH₂CH₃ H O 0 A-0826 H H H H H CH(CH₃)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0827 H H H H H CH₂C(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0828 H H H H H CH₂(CH₂)₂CH₃ CH₂CH₂CH₃ H O 0 A-0829 H H H H H CH₂(CH₂)₃CH₃ CH₂CH₂CH₃ H O 0 A-0830 H H H H H CH₂(CH₂)₄CH₃ CH₂CH₂CH₃ H O 0 A-0831 H H H H H CH₂(CH₂)₆CH₃ CH₂CH₂CH₃ H O 0 A-0832 H H H H H CH₂OCH₃ CH₂CH₂CH₃ H O 0 A-0833 H H H H H CH₂OCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0834 H H H H H CH₂CH₂OCH₃ CH₂CH₂CH₃ H O 0 A-0835 H H H H H CH₂CH₂OCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0836 H H H H H CF₃ CH₂CH₂CH₃ H O 0 A-0837 H H H H H CHF₂ CH₂CH₂CH₃ H O 0 A-0838 H H H H H CH₂CF₃ CH₂CH₂CH₃ H O 0 A-0839 H H H H H CH₂CHF₂ CH₂CH₂CH₃ H O 0 A-0840 H H H H H CH₂CClF₂ CH₂CH₂CH₃ H O 0 A-0841 H H H H H CH₂CBrF₂ CH₂CH₂CH₃ H O 0 A-0842 H H H H H CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0843 H H H H H CF₂CHF₂ CH₂CH₂CH₃ H O 0 A-0844 H H H H H CH₂CH₂CF₃ CH₂CH₂CH₃ H O 0 A-0845 H H H H H CH₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0846 H H H H H CH₂CF₂CHF₂ CH₂CH₂CH₃ H O 0 A-0847 H H H H H CF₂CHFCF₃ CH₂CH₂CH₃ H O 0 A-0848 H H H H H CF₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0849 H H H H H CH₂CF₂CF₂CF₃ CH₂CH₂CH₃ H O 0

TABLE 15 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0850 H H H H H CH₂CF₂CHFCF₃ CH₂CH₂CH₃ H O 0 A-0851 H H H H H CH₂CH₂CH₂CF₃ CH₂CH₂CH₃ H O 0 A-0852 H H H H H CH₂CH₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0853 H H H H H CF₂CF₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0854 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CH₂CH₃ H O 0 A-0855 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0856 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0857 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₂CH₃ H O 0 A-0858 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₂CH₃ H O 0 A-0859 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₂CH₃ H O 0 A-0860 H H H H H CF₂CHFOCH₃ CH₂CH₂CH₃ H O 0 A-0861 H H H H H CF₂CHFOCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0862 H H H H H CH₂CH₂OCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0863 H H H H H CF₂CHFOCF₃ CH₂CH₂CH₃ H O 0 A-0864 H H H H H CF₂CHFOCF₂CF₃ CH₂CH₂CH₃ H O 0 A-0865 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₂CH₂CH₃ H O 0 A-0866 H H H H H CH₂CH═CH₂ CH₂CH₂CH₃ H O 0 A-0867 H H H H H CH₂CH═CHCl CH₂CH₂CH₃ H O 0 A-0868 H H H H H CH₂CH═CCl₂ CH₂CH₂CH₃ H O 0 A-0869 H H H H H CH₂CH₂CF═CF₂ CH₂CH₂CH₃ H O 0 A-0870 H H H H H CH₂CH₂CH═CF₂ CH₂CH₂CH₃ H O 0 A-0871 H H H H H CH₂C≡CH CH₂CH₂CH₃ H O 0 A-0872 H H H H H CH₂C≡CCH₃ CH₂CH₂CH₃ H O 0 A-0873 H H H H H CH₂C≡CI CH₂CH₂CH₃ H O 0 A-0874 H H H H H CH₂C≡CCF₃ CH₂CH₂CH₃ H O 0 A-0875 H H H H H cyclobutyl CH₂CH₂CH₃ H O 0 A-0876 H H H H H cyclopentyl CH₂CH₂CH₃ H O 0 A-0877 H H H H H cyclohexyl CH₂CH₂CH₃ H O 0 A-0878 H H H H H 4,4-difluorocyclohexyl CH₂CH₂CH₃ H O 0 A-0879 H H H H H CH₂(cyclopropyl) CH₂CH₂CH₃ H O 0 A-0880 H H H H H CH₂(cyclobutyl) CH₂CH₂CH₃ H O 0 A-0881 H H H H H CH₂(cyclopentyl) CH₂CH₂CH₃ H O 0 A-0882 H H H H H CH₂CH₂(cyclopropyl) CH₂CH₂CH₃ H O 0 A-0883 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₂CH₃ H O 0 A-0884 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₂CH₃ H O 0 A-0885 H H H H H CH₂(4,4-difluorocyclohexyl) CH₂CH₂CH₃ H O 0 A-0886 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₂CH₃ H O 0 A-0887 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₂CH₃ H O 0 A-0888 H H H H H CH₂SCH₃ CH₂CH₂CH₃ H O 0 A-0889 H H H H H CH₂SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0890 H H H H H CH₂CH₂SCH₃ CH₂CH₂CH₃ H O 0 A-0891 H H H H H CH₂CH₂SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0892 H H H H H CH₂CH₂CH₂SCH₃ CH₂CH₂CH₃ H O 0 A-0893 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0894 H H H H H CH(CH₃)SCH₃ CH₂CH₂CH₃ H O 0 A-0895 H H H H H CH(CH₃)SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0896 H H H H H CH₂CH(CH₃)SCH₃ CH₂CH₂CH₃ H O 0 A-0897 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0898 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₂CH₃ H O 0 A-0899 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0900 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₂CH₃ H O 0 A-0901 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0902 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₂CH₃ H O 0 A-0903 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0904 H H H H H CH₂SOCH₃ CH₂CH₂CH₃ H O 0 A-0905 H H H H H CH₂CH₂SOCH₃ CH₂CH₂CH₃ H O 0 A-0906 H H H H H CH₂CH₂CH₂SOCH₃ CH₂CH₂CH₃ H O 0 A-0907 H H H H H CH(CH₃)SOCH₃ CH₂CH₂CH₃ H O 0 A-0908 H H H H H CH₂CH(CH₃)SOCH₃ CH₂CH₂CH₃ H O 0 A-0909 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₂CH₃ H O 0 A-0910 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₂CH₃ H O 0

TABLE 16 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0911 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₂CH₃ H O 0 A-0912 H H H H H CH₂SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0913 H H H H H CH₂CH₂SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0914 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0915 H H H H H CH(CH₃)SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0916 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0917 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0918 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0919 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₂CH₃ H O 0 A-0920 H H H H H CH₂SCF₃ CH₂CH₂CH₃ H O 0 A-0921 H H H H H CH₂SCHF₂ CH₂CH₂CH₃ H O 0 A-0922 H H H H H CH₂SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0923 H H H H H CH₂SCH₂CHF₂ CH₂CH₂CH₃ H O 0 A-0924 H H H H H CH₂SCF₂CF₃ CH₂CH₂CH₃ H O 0 A-0925 H H H H H CH₂CH₂SCF₃ CH₂CH₂CH₃ H O 0 A-0926 H H H H H CH₂CH₂SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0927 H H H H H CH₂CH₂CH₂SCF₃ CH₂CH₂CH₃ H O 0 A-0928 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0929 H H H H H CH(CH₃)SCF₃ CH₂CH₂CH₃ H O 0 A-0930 H H H H H CH(CH₃)SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0931 H H H H H CH₂CH(CH₃)SCF₃ CH₂CH₂CH₃ H O 0 A-0932 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0933 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₂CH₃ H O 0 A-0934 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0935 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₂CH₃ H O 0 A-0936 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0937 H H H H H CH₂CH₂CH(CH)SCF₃ CH₂CH₂CH₃ H O 0 A-0938 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0939 H H H H H CH₂SOCF₃ CH₂CH₂CH₃ H O 0 A-0940 H H H H H CH₂CH₂SOCF₃ CH₂CH₂CH₃ H O 0 A-0941 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CH₂CH₃ H O 0 A-0942 H H H H H CH(CH₃)SOCF₃ CH₂CH₂CH₃ H O 0 A-0943 H H H H H CH₂CH(CH₃)SOCF₃ CH₂CH₂CH₃ H O 0 A-0944 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₂CH₃ H O 0 A-0945 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₂CH₃ H O 0 A-0946 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₂CH₃ H O 0 A-0947 H H H H H CH₂SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0948 H H H H H CH₂CH₂SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0949 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0950 H H H H H CH(CH₃)SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0951 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0952 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0953 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0954 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₂CH₃ H O 0 A-0955 H H H H H CH₂C(═O)CH₃ CH₂CH₂CH₃ H O 0 A-0956 H H H H H CH₂C(═O)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0957 H H H H H CH₂C(═O)C(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0958 H H H H H CH₂CH₂C(═O)CH₃ CH₂CH₂CH₃ H O 0 A-0959 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0960 H H H H H CH₂C(═O)CF₃ CH₂CH₂CH₃ H O 0 A-0961 H H H H H CH₂CH₂C(═O)CF₃ CH₂CH₂CH₃ H O 0 A-0962 H H H H H CH₂C(═O)OCH₃ CH₂CH₂CH₃ H O 0 A-0963 H H H H H CH₂C(═O)OCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0964 H H H H H CH₂C(═O)OC(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0965 H H H H H CH₂CH₂C(═O)OCH₃ CH₂CH₂CH₃ H O 0 A-0966 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₂CH₃ H O 0 A-0967 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0968 H H H H H CH₂C(═O)NH₂ CH₂CH₂CH₃ H O 0 A-0969 H H H H H CH₂CH₂C(═O)NH₂ CH₂CH₂CH₃ H O 0 A-0970 H H H H H CH₂C(═O)NHCH₃ CH₂CH₂CH₃ H O 0 A-0971 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₂CH₃ H O 0

TABLE 17 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-0972 H H H H H CH₂CH₂C(═O)NHCH₃ CH₂CH₂CH₃ H O 0 A-0973 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₂CH₃ H O 0 A-0974 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₂CH₃ H O 0 A-0975 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0976 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₂CH₃ H O 0 A-0977 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₂CH₃ H O 0 A-0978 H H H H H CH₂C(═O)N(CH3)₂ CH₂CH₂CH₃ H O 0 A-0979 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₂CH₃ H O 0 A-0980 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₂CH₃ H O 0 A-0981 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₂CH₃ H O 0 A-0982 H H H H H CH₂CH₂OH CH₂CH₂CH₃ H O 0 A-0983 H H H H H CH₂CH(OH)CH₃ CH₂CH₂CH₃ H O 0 A-0984 H H H H H CH₂CH₂CH₂OH CH₂CH₂CH₃ H O 0 A-0985 H H H H H CH₂CH(OH)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0986 H H H H H CH₂CH(OH)C(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0987 H H H H H CH₂CH₂CH(OH)CH₃ CH₂CH₂CH₃ H O 0 A-0988 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0989 H H H H H CH₂C(═NOH)CH₃ CH₂CH₂CH₃ H O 0 A-0990 H H H H H CH₂C(═NOH)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0991 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₂CH₂CH₃ H O 0 A-0992 H H H H H CH₂C(═NOCH₃)CH₃ CH₂CH₂CH₃ H O 0 A-0993 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0994 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₂CH₃ H O 0 A-0995 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0996 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₂CH₃ H O 0 A-0997 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₂CH₃ H O 0 A-0998 H H H H H CH₂Ph CH₂CH₂CH₃ H O 0 A-0999 H H H H H CH₂(2-F)Ph CH₂CH₂CH₃ H O 0 A-1000 H H H H H CH₂(3-F)Ph CH₂CH₂CH₃ H O 0 A-1001 H H H H H CH₂(4-F)Ph CH₂CH₂CH₃ H O 0 A-1002 H H H H H CH₂(2-Cl)Ph CH₂CH₂CH₃ H O 0 A-1003 H H H H H CH₂(3-Cl)Ph CH₂CH₂CH₃ H O 0 A-1004 H H H H H CH₂(4-O)Ph CH₂CH₂CH₃ H O 0 A-1005 H H H H H CH₂(2-CF₃)Ph CH₂CH₂CH₃ H O 0 A-1006 H H H H H CH₂(3-CF₃)Ph CH₂CH₂CH₃ H O 0 A-1007 H H H H H CH₂(4-CF₃)Ph CH₂CH₂CH₃ H O 0 A-1008 H H H H H CH₂(naphthalen-1-yl) CH₂CH₂CH₃ H O 0 A-1009 H H H H H CH₂(naphthalen-2-yl) CH₂CH₂CH₃ H O 0 A-1010 H H H H H CH₂CH₂Ph CH₂CH₂CH₃ H O 0 A-1011 H H H H H H cyclopropyl H O 0 A-1012 H H H H H CH₃ cyclopropyl H O 0 A-1013 H H H H H CH₂CH₃ cyclopropyl H O 0 A-1014 H H H H H CH(CH₃)₂ cyclopropyl H O 0 A-1015 H H H H H CH₂CH₂CH₃ cyclopropyl H O 0 A-1016 H H H H H CH₂CH(CH₃)₂ cyclopropyl H O 0 A-1017 H H H H H CH(CH₃)CH₂CH₃ cyclopropyl H O 0 A-1018 H H H H H CH₂C(CH₃)₃ cyclopropyl H O 0 A-1019 H H H H H CH₂(CH₂)₂CH₃ cyclopropyl H O 0 A-1020 H H H H H CH₂(CH₂)₃CH₃ cyclopropyl H O 0 A-1021 H H H H H CF₃ cyclopropyl H O 0 A-1022 H H H H H CHF₂ cyclopropyl H O 0 A-1023 H H H H H CH₂CF₃ cyclopropyl H O 0 A-1024 H H H H H CH₂CHF₂ cyclopropyl H O 0 A-1025 H H H H H CH₂CClF₂ cyclopropyl H O 0 A-1026 H H H H H CH₂CBrF₂ cyclopropyl H O 0 A-1027 H H H H H CF₂CF₃ cyclopropyl H O 0 A-1028 H H H H H CF₂CHF₂ cyclopropyl H O 0 A-1029 H H H H H CH₂CH₂CF₃ cyclopropyl H O 0 A-1030 H H H H H CH₂CF₂CF₃ cyclopropyl H O 0 A-1031 H H H H H CH₂CF₂CHF₂ cyclopropyl H O 0 A-1032 H H H H H CF₂CHFCF₃ cyclopropyl H O 0

TABLE 18 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1033 H H H H H CF₂CF₂CF₃ cyclopropyl H O 0 A-1034 H H H H H CH₂CF₂CF₂CF₃ cyclopropyl H O 0 A-1035 H H H H H CH₂CF₂CHFCF₃ cyclopropyl H O 0 A-1036 H H H H H CH₂CH₂CH₂CF₃ cyclopropyl H O 0 A-1037 H H H H H CH₂CH₂CF₂CF₃ cyclopropyl H O 0 A-1038 H H H H H CF₂CF₂CF₂CF₃ cyclopropyl H O 0 A-1039 H H H H H CH₂CH₂CH(CF₃)₂ cyclopropyl H O 0 A-1040 H H H H H CF₂CF₂CF₂CF₂CF₃ cyclopropyl H O 0 A-1041 H H H H H CH₂CF₂CF₂CF₂CF₃ cyclopropyl H O 0 A-1042 H H H H H CH₂CH₂CH₂CH₂CF₃ cyclopropyl H O 0 A-1043 H H H H H CH₂CF₂CF₂CF₂CHF₂ cyclopropyl H O 0 A-1044 H H H H H CH₂CH₂OCH₂CF₃ cyclopropyl H O 0 A-1045 H H H H H CF₂CHFOCF₃ cyclopropyl H O 0 A-1046 H H H H H CF₂CHFOCF₂CF₃ cyclopropyl H O 0 A-1047 H H H H H CH₂CH₂CF═CF₂ cyclopropyl H O 0 A-1048 H H H H H CH₂CH₂CH═CF₂ cyclopropyl H O 0 A-1049 H H H H H CH₂C≡CCH₃ cyclopropyl H O 0 A-1050 H H H H H CH₂C≡CCF₃ cyclopropyl H O 0 A-1051 H H H H H CH₂C≡CI cyclopropyl H O 0 A-1052 H H H H H CH₂(2,2-difluorocyclopropyl) cyclopropyl H O 0 A-1053 H H H H H CH₂(2,2-dichlorocyclopropyl) cyclopropyl H O 0 A-1054 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) cyclopropyl H O 0 A-1055 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) cyclopropyl H O 0 A-1056 H H H H H CH₂SCH₃ cyclopropyl H O 0 A-1057 H H H H H CH₂SCH₂CH₃ cyclopropyl H O 0 A-1058 H H H H H CH₂CH₂SCH₃ cyclopropyl H O 0 A-1059 H H H H H CH₂SOCH₃ cyclopropyl H O 0 A-1060 H H H H H CH₂CH₂SOCH₃ cyclopropyl H O 0 A-1061 H H H H H CH₂SO₂CH₃ cyclopropyl H O 0 A-1062 H H H H H CH₂CH₂SO₂CH₃ cyclopropyl H O 0 A-1063 H H H H H CH₂SCF₃ cyclopropyl H O 0 A-1064 H H H H H CH₂SCHF₂ cyclopropyl H O 0 A-1065 H H H H H CH₂SCH₂CF₃ cyclopropyl H O 0 A-1066 H H H H H CH₂SCH₂CHF₂ cyclopropyl H O 0 A-1067 H H H H H CH₂SCF₂CF₃ cyclopropyl H O 0 A-1068 H H H H H CH₂CH₂SCF₃ cyclopropyl H O 0 A-1069 H H H H H CH₂SOCF₃ cyclopropyl H O 0 A-1070 H H H H H CH₂CH₂SOCF₃ cyclopropyl H O 0 A-1071 H H H H H CH₂CH₂CH₂SOCF₃ cyclopropyl H O 0 A-1072 H H H H H CH₂SO₂CF₃ cyclopropyl H O 0 A-1073 H H H H H CH₂CH₂SO₂CF₃ cyclopropyl H O 0 A-1074 H H H H H CH₂CH₂CH₂SO₂CF₃ cyclopropyl H O 0 A-1075 H H H H H CH₂C(═O)NHCH₂CHF₂ cyclopropyl H O 0 A-1076 H H H H H CH₂C(═O)NHCH₂CF₃ cyclopropyl H O 0 A-1077 H H H H H H CH₂C≡CH H O 0 A-1078 H H H H H CH₃ CH₂C≡CH H O 0 A-1079 H H H H H CH₂CH₃ CH₂C≡CH H O 0 A-1080 H H H H H CH(CH₃)₂ CH₂C≡CH H O 0 A-1081 H H H H H CH₂CH₂CH₃ CH₂C≡CH H O 0 A-1082 H H H H H CH₂CH(CH₃)₂ CH₂C≡CH H O 0 A-1083 H H H H H CH(CH₃)CH₂CH₃ CH₂C≡CH H O 0 A-1084 H H H H H CH₂C(CH₃)₃ CH₂C≡CH H O 0 A-1085 H H H H H CH₂(CH₂)₂CH₃ CH₂C≡CH H O 0 A-1086 H H H H H CH₂(CH₂)₃CH₃ CH₂C≡CH H O 0 A-1087 H H H H H CH₂(CH2)₄CH₃ CH₂C≡CH H O 0 A-1088 H H H H H CH₂(CH₂)₆CH₃ CH₂C≡CH H O 0 A-1089 H H H H H CH₂OCH₃ CH₂C≡CH H O 0 A-1090 H H H H H CH₂OCH₂CH₃ CH₂C≡CH H O 0 A-1091 H H H H H CH₂CH₂OCH₃ CH₂C≡CH H O 0 A-1092 H H H H H CH₂CH₂OCH₂CH₃ CH₂C≡CH H O 0 A-1093 H H H H H CF₃ CH₂C≡CH H O 0

TABLE 19 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1094 H H H H H CHF₂ CH₂C≡CH H O 0 A-1095 H H H H H CH₂CF₃ CH₂C≡CH H O 0 A-1096 H H H H H CH₂CHF₂ CH₂C≡CH H O 0 A-1097 H H H H H CH₂CClF₂ CH₂C≡CH H O 0 A-1098 H H H H H CH₂CBrF₂ CH₂C≡CH H O 0 A-1099 H H H H H CF₂CF₃ CH₂C≡CH H O 0 A-1100 H H H H H CF₂CHF₂ CH₂C≡CH H O 0 A-1101 H H H H H CH₂CH₂CF₃ CH₂C≡CH H O 0 A-1102 H H H H H CH₂CF₂CF₃ CH₂C≡CH H O 0 A-1103 H H H H H CH₂CF₂CHF₂ CH₂C≡CH H O 0 A-1104 H H H H H CF₂CHFCF₃ CH₂C≡CH H O 0 A-1105 H H H H H CF₂CF₂CF₃ CH₂C≡CH H O 0 A-1106 H H H H H CH₂CF₂CF₂CF₃ CH₂C≡CH H O 0 A-1107 H H H H H CH₂CF₂CHFCF₃ CH₂C≡CH H O 0 A-1108 H H H H H CH₂CH₂CH₂CF₃ CH₂C≡CH H O 0 A-1109 H H H H H CH₂CH₂CF₂CF₃ CH₂C≡CH H O 0 A-1110 H H H H H CF₂CF₂CF₂CF₃ CH₂C≡CH H O 0 A-1111 H H H H H CH₂CH₂CH(CF₃)₂ CH₂C≡CH H O 0 A-1112 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂C≡CH H O 0 A-1113 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂C≡CH H O 0 A-1114 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂C≡CH H O 0 A-1115 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂C≡CH H O 0 A-1116 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂C≡CH H O 0 A-1117 H H H H H CF₂CHFOCH₃ CH₂C≡CH H O 0 A-1118 H H H H H CF₂CHFOCH₂CH₃ CH₂C≡CH H O 0 A-1119 H H H H H CH₂CH₂OCH₂CF₃ CH₂C≡CH H O 0 A-1120 H H H H H CF₂CHFOCF₃ CH₂C≡CH H O 0 A-1121 H H H H H CF₂CHFOCF₂CF₃ CH₂C≡CH H O 0 A-1122 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₂C≡CH H O 0 A-1123 H H H H H CH₂CH═CH₂ CH₂C≡CH H O 0 A-1124 H H H H H CH₂CH═CHCl CH₂C≡CH H O 0 A-1125 H H H H H CH₂CH═CCl₂ CH₂C≡CH H O 0 A-1126 H H H H H CH₂CH₂CF═CF₂ CH₂C≡CH H O 0 A-1127 H H H H H CH₂CH₂CH═CF₂ CH₂C≡CH H O 0 A-1128 H H H H H CH₂C≡CH CH₂C≡CH H O 0 A-1129 H H H H H CH₂C≡CCH₃ CH₂C≡CH H O 0 A-1130 H H H H H CH₂C≡CCF₃ CH₂C≡CH H O 0 A-1131 H H H H H CH₂C≡CI CH₂C≡CH H O 0 A-1132 H H H H H cyclobutyl CH₂C≡CH H O 0 A-1133 H H H H H cyclopentyl CH₂C≡CH H O 0 A-1134 H H H H H cyclohexyl CH₂C≡CH H O 0 A-1135 H H H H H 4,4-difluorocycyohexyl CH₂C≡CH H O 0 A-1136 H H H H H CH₂(cyclopropyl) CH₂C≡CH H O 0 A-1137 H H H H H CH₂(cyclobutyl) CH₂C≡CH H O 0 A-1138 H H H H H CH₂(cyclopentyl) CH₂C≡CH H O 0 A-1139 H H H H H CH₂CH₂(cyclopropyl) CH₂C≡CH H O 0 A-1140 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂C≡CH H O 0 A-1141 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂C≡CH H O 0 A-1142 H H H H H CH₂(4,4-difluorocyclohexyl) CH₂C≡CH H O 0 A-1143 H H H H H CH₂CH₂(2,2- CH₂C≡CH H O 0 difluorocyclopropyl) A-1144 H H H H H CH₂CH₂(2,2- CH₂C≡CH H O 0 dichlorocyclopropyl) A-1145 H H H H H CH₂SCH₃ CH₂C≡CH H O 0 A-1146 H H H H H CH₂SCH₂CH₃ CH₂C≡CH H O 0 A-1147 H H H H H CH₂CH₂SCH₃ CH₂C≡CH H O 0 A-1148 H H H H H CH₂CH₂SCH₂CH₃ CH₂C≡CH H O 0 A-1149 H H H H H CH₂CH₂CH₂SCH₃ CH₂C≡CH H O 0 A-1150 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂C≡CH H O 0 A-1151 H H H H H CH(CH₃)SCH₃ CH₂C≡CH H O 0 A-1152 H H H H H CH(CH₃)SCH₂CH₃ CH₂C≡CH H O 0 A-1153 H H H H H CH₂CH(CH₃)SCH₃ CH₂C≡CH H O 0 A-1154 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂C≡CH H O 0

TABLE 20 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1155 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₂C≡CH H O 0 A-1156 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂C≡CH H O 0 A-1157 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂C≡CH H O 0 A-1158 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂C≡CH H O 0 A-1159 H H H H H CH₂CH₂CH(CH)SCH₃ CH₂C≡CH H O 0 A-1160 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂C≡CH H O 0 A-1161 H H H H H CH₂SOCH₃ CH₂C≡CH H O 0 A-1162 H H H H H CH₂CH₂SOCH₃ CH₂C≡CH H O 0 A-1163 H H H H H CH₂CH₂CH₂SOCH₃ CH₂C≡CH H O 0 A-1164 H H H H H CH(CH₃)SOCH₃ CH₂C≡CH H O 0 A-1165 H H H H H CH₂CH(CH₃)SOCH₃ CH₂C≡CH H O 0 A-1166 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂C≡CH H O 0 A-1167 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂C≡CH H O 0 A-1168 H H H H H CH₂CH₂CH(OH₃)SOCH₃ CH₂C≡CH H O 0 A-1169 H H H H H CH₂SO₂CH₃ CH₂C≡CH H O 0 A-1170 H H H H H CH₂CH₂SO₂CH₃ CH₂C≡CH H O 0 A-1171 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₂C≡CH H O 0 A-1172 H H H H H CH(CH₃)SO₂CH₃ CH₂C≡CH H O 0 A-1173 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₂C≡CH H O 0 A-1174 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂C≡CH H O 0 A-1175 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂C≡CH H O 0 A-1176 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂C≡CH H O 0 A-1177 H H H H H CH₂SCF₃ CH₂C≡CH H O 0 A-1178 H H H H H CH₂SCHF₂ CH₂C≡CH H O 0 A-1179 H H H H H CH₂SCH₂CF₃ CH₂C≡CH H O 0 A-1180 H H H H H CH₂SCH₂CHF₂ CH₂C≡CH H O 0 A-1181 H H H H H CH₂SCF₂CF₃ CH₂C≡CH H O 0 A-1182 H H H H H CH₂CH₂SCF₃ CH₂C≡CH H O 0 A-1183 H H H H H CH₂CH₂SCH₂CF₃ CH₂C≡CH H O 0 A-1184 H H H H H CH₂CH₂CH₂SCF₃ CH₂C≡CH H O 0 A-1185 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂C≡CH H O 0 A-1186 H H H H H CH(CH₃)SCF₃ CH₂C≡CH H O 0 A-1187 H H H H H CH(CH₃)SCH₂CF₃ CH₂C≡CH H O 0 A-1188 H H H H H CH₂CH(CH₃)SCF₃ CH₂C≡CH H O 0 A-1189 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂C≡CH H O 0 A-1190 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂C≡CH H O 0 A-1191 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂C≡CH H O 0 A-1192 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂C≡CH H O 0 A-1193 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂C≡CH H O 0 A-1194 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₂C≡CH H O 0 A-1195 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂C≡CH H O 0 A-1196 H H H H H CH₂SOCF₃ CH₂C≡CH H O 0 A-1197 H H H H H CH₂CH₂SOCF₃ CH₂C≡CH H O 0 A-1198 H H H H H CH₂CH₂CH₂SOCF₃ CH₂C≡CH H O 0 A-1199 H H H H H CH(CH₃)SOCF₃ CH₂C≡CH H O 0 A-1200 H H H H H CH₂CH(CH₃)SOCF₃ CH₂C≡CH H O 0 A-1201 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂C≡CH H O 0 A-1202 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂C≡CH H O 0 A-1203 H H H H H CH₂CH2CH(CH₃)SOCF₃ CH₂C≡CH H O 0 A-1204 H H H H H CH₂SO₂CF₃ CH₂C≡CH H O 0 A-1205 H H H H H CH₂CH₂SO₂CF₃ CH₂C≡CH H O 0 A-1206 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂C≡CH H O 0 A-1207 H H H H H CH(CH₃)SO₂CF₃ CH₂C≡CH H O 0 A-1208 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₂C≡CH H O 0 A-1209 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂C≡CH H O 0 A-1210 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂C≡CH H O 0 A-1211 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂C≡CH H O 0 A-1212 H H H H H CH₂C(═O)CH₃ CH₂C≡CH H O 0 A-1213 H H H H H CH₂C(═O)CH₂CH₃ CH₂C≡CH H O 0 A-1214 H H H H H CH₂C(═O)C(CH₃)₃ CH₂C≡CH H O 0 A-1215 H H H H H CH₂CH₂C(═O)CH₃ CH₂C≡CH H O 0

TABLE 21 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1216 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂C≡CH H O 0 A-1217 H H H H H CH₂C(═O)CF₃ CH₂C≡CH H O 0 A-1218 H H H H H CH₂CH₂C(═O)CF₃ CH₂C≡CH H O 0 A-1219 H H H H H CH₂C(═O)OCH₃ CH₂C≡CH H O 0 A-1220 H H H H H CH₂C(═O)OCH₂CH₃ CH₂C≡CH H O 0 A-1221 H H H H H CH₂C(═O)OC(CH₃)₃ CH₂C≡CH H O 0 A-1222 H H H H H CH₂CH₂C(═O)OCH₃ CH₂C≡CH H O 0 A-1223 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂C≡CH H O 0 A-1224 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂C≡CH H O 0 A-1225 H H H H H CH₂C(═O)NH₂ CH₂C≡CH H O 0 A-1226 H H H H H CH₂CH₂C(═O)NH₂ CH₂C≡CH H O 0 A-1227 H H H H H CH₂C(═O)NHCH₃ CH₂C≡CH H O 0 A-1228 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₂C≡CH H O 0 A-1229 H H H H H CH₂CH₂C(═O)NHCH₃ CH₂C≡CH H O 0 A-1230 H H H H H CH₂CH,C(═O)NHCH(CH₃)₂ CH₂C≡CH H O 0 A-1231 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂C≡CH H O 0 A-1232 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂C≡CH H O 0 A-1233 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂C≡CH H O 0 A-1234 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂C≡CH H O 0 A-1235 H H H H H CH₂C(═O)N(CH₃)₂ CH₂C≡CH H O 0 A-1236 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂C≡CH H O 0 A-1237 H H H H H CH₂CH₂C(═O)N(CH3)₂ CH₂C≡CH H O 0 A-1238 H H H H H CH₂CH₂C(═O)N(CH₂CH3)₂ CH₂C≡CH H O 0 A-1239 H H H H H CH₂CH₂OH CH₂C≡CH H O 0 A-1240 H H H H H CH₂CH(OH)CH₃ CH₂C≡CH H O 0 A-1241 H H H H H CH₂CH2CH₂OH CH₂C≡CH H O 0 A-1242 H H H H H CH₂CH(OH)CH₂CH₃ CH₂C≡CH H O 0 A-1243 H H H H H CH₂CH(OH)C(CH₃)₃ CH₂C≡CH H O 0 A-1244 H H H H H CH₂CH₂CH(OH)CH₃ CH₂C≡CH H O 0 A-1245 H H H H H CH₂CH₂CH(OH)C(CH3)₃ CH₂C≡CH H O 0 A-1246 H H H H H CH₂C(═NOH)CH₃ CH₂C≡CH H O 0 A-1247 H H H H H CH₂C(═NOH)CH₂CH₃ CH₂C≡CH H O 0 A-1248 H H H H H CH₂C(═NOH)C(CH₂)₃ CH₂C≡CH H O 0 A-1249 H H H H H CH₂C(═NOCH₃)CH₃ CH₂C≡CH H O 0 A-1250 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂C≡CH H O 0 A-1251 H H H H H CH₂C(═NOCH₂CH₃)CH3 CH₂C≡CH H O 0 A-1252 H H H H H CH₂C(═NOCHXH₃)CH₂CH₃ CH₂C≡CH H O 0 A-1253 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂C≡CH H O 0 A-1254 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂C≡CH H O 0 A-1255 H H H H H CH₂Ph CH₂C≡CH H O 0 A-1256 H H H H H CH₂(2-F)Ph CH₂C≡CH H O 0 A-1257 H H H H H CH₂(3-F)Ph CH₂C≡CH H O 0 A-1258 H H H H H CH₂(4-F)Ph CH₂C≡CH H O 0 A-1259 H H H H H CH₂(2-Cl)Ph CH₂C≡CH H O 0 A-1260 H H H H H CH₂(3-Cl)Ph CH₂C≡CH H O 0 A-1261 H H H H H CH₂(4-Cl)Ph CH₂C≡CH H O 0 A-1262 H H H H H CH₂(2-CF₃)Ph CH₂C≡CH H O 0 A-1263 H H H H H CH₂(3-CF₃)Ph CH₂C≡CH H O 0 A-1264 H H H H H CH₂(4-CF₃)Ph CH₂C≡CH H O 0 A-1265 H H H H H CH₂(naphthalen-1-y1) CH₂C≡CH H O 0 A-1266 H H H H H CH7(naplithalen-2-y1) CH₂C≡CH H O 0 A-1267 H H H H H CH₂CH₂Ph CH₂C≡CH H O 0 A-1268 H H H H H H OH H O 0 A-1269 H H H H H CH₃ OH H O 0 A-1270 H H H H H CH₂CH₃ OH H O 0 A-1271 H H H H H CH(CH₃)₂ OH H O 0 A-1272 H H H H H CH₂CH₂CH₃ OH H O 0 A-1273 H H H H H CH₂CH(CH₃)₂ OH H O 0 A-1274 H H H H H CH(CH₃)CH₂CH₃ OH H O 0 A-1275 H H H H H CH₂C(CH₃)₃ OH H O 0 A-1276 H H H H H CH₂(CH₂)₂CH₂ OH H O 0

TABLE 22 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1277 H H H H H CH₂(CH₂)₃CH₃ OH H O 0 A-1278 H H H H H CF₃ OH H O 0 A-1279 H H H H H CHF₂ OH H O 0 A-1280 H H H H H CH₂CF₃ OH H O 0 A-1281 H H H H H CH₂CHF₂ OH H O 0 A-1282 H H H H H CH₂CClF₂ OH H O 0 A-1283 H H H H H CH₂CBrF₂ OH H O 0 A-1284 H H H H H CF₂CF₃ OH H O 0 A-1285 H H H H H CF₂CHF₂ OH H O 0 A-1286 H H H H H CH₂CH₂CF₃ OH H O 0 A-1287 H H H H H CH₂CH₂CF₃ OH H O 0 A-1288 H H H H H CH₂CF₂CHF₂ OH H O 0 A-1289 H H H H H CF₂CHFCF₃ OH H O 0 A-1290 H H H H H CF₂CF₂CF₃ OH H O 0 A-1291 H H H H H CH₂CF₂CF₂CF₃ OH H O 0 A-1292 H H H H H CH₂CF₂CHFCF₃ OH H O 0 A-1293 H H H H H CH₂CH₂CH₂SF₃ OH H O 0 A-1294 H H H H H CH₂CH₂CF₂CF₃ OH H O 0 A-1295 H H H H H CF₂CF₂CF₂CF₃ OH H O 0 A-1296 H H H H H CH₂CH₂CH(CF₃)₂ OH H O 0 A-1297 H H H H H CF₂CFCF₂CF₂CF₃ OH H O 0 A-1298 H H H H H CH₂CF₂CF₂CF₂CF₃ OH H O 0 A-1299 H H H H H CH₂CH₂OH₂CH₂OF₃ OH H O 0 A-1300 H H H H H CH₂CF₂CF₂CF₂CHF₂ OH H O 0 A-1301 H H H H H CH₂CH₂OCH₂CF₃ OH H O 0 A-1302 H H H H H CF₂CHFOOF₃ OH H O 0 A-1303 H H H H H CF₂CHFOCF₂CF₃ OH H O 0 A-1304 H H H H H CH₂CH₂CF═CF₂ OH H O 0 A-1305 H H H H H CH₂CH₂CH═CF₂ OH H O 0 A-1306 H H H H H CH₂C≡CCH₃ OH H O 0 A-1307 H H H H H CH₂C≡CCF₃ OH H O 0 A-1308 H H H H H CH₂C≡CI OH H O 0 A-1309 H H H H H CH₂(2,2- OH H O 0 difluorocyclopropyl) A-1310 H H H H H CH₂(2,2- OH H O 0 dichlorocyclopropyl) A-1311 H H H H H CH₂CH₂(2,2- OH H O 0 diftuorocyclopropyl) A-1312 H H H H H CH₂CH₂(2,2- OH H O 0 dichlorocyclopropyl) A-1313 H H H H H CH₂SCH₂ OH H O 0 A-1314 H H H H H CH₂SCH₂CH₃ OH H O 0 A-1315 H H H H H CH₂CH₂SCH₃ OH H O 0 A-1316 H H H H H CH₂SOCH₃ OH H O 0 A-1317 H H H H H CH₂CH₂SOCH₃ OH H O 0 A-1318 H H H H H CH₂SO₂CH₃ OH H O 0 A-1319 H H H H H CH₂CH₂SO₂CH₃ OH H O 0 A-1320 H H H H H CH₂SCF₃ OH H O 0 A-1321 H H H H H CH₂SCHF₂ OH H O 0 A-1322 H H H H H CH₂SCH₂CF₂ OH H O 0 A-1323 H H H H H CH₂SCH₂CHF₂ OH H O 0 A-1324 H H H H H CH₂SCF₂CF₃ OH H O 0 A-1325 H H H H H CH₂CH₂SCF₂ OH H O 0 A-1326 H H H H H CH₂SOCF₂ OH H O 0 A-1327 H H H H H CH₂CH₂SOCF₃ OH H O 0 A-1328 H H H H H CH₂CH₂CH₂SOCF₃ OH H O 0 A-1329 H H H H H CH₂SO₂CF₃ OH H O 0 A-1330 H H H H H CH₂CH₂SO₂CF₃ OH H O 0 A-1331 H H H H H CH₂CH₂CH₂SO₂CF₃ OH H O 0 A-1332 H H H H H CH₂C(═O)NNCH₂CHF₂ OH H O 0 A-1333 H H H H H CH₂C(═O)NNCH₂CF₂ OH H O 0 A-1334 H H H H H H OH H O 0 A-1335 H H H H H CH₃ OH H O 0 A-1336 H H H H H CH₂CH₃ OH H O 0 A-1337 H H H H H CH(CH₃)₂ OH H O 0

TABLE 23 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1338 H H H H H CH₂CH₂CH₃ OCH₃ H O 0 A-1339 H H H H H CH₂CH(CH₃)₂ OCH₃ H O 0 A-1340 H H H H H CH(CH₃)CH₂CH₃ OCH₃ H O 0 A-1341 H H H H H CH₂C(CH₃)₃ OCH₃ H O 0 A-1342 H H H H H CH₂(CH₂)₂CH₃ OCH₃ H O 0 A-1343 H H H H H CH₂(CH₂)₃CH₃ OCH₃ H O 0 A-1344 H H H H H CF₃ OCH₃ H O 0 A-1345 H H H H H CHF₂ OCH₃ H O 0 A-1346 H H H H H CH₂CF₃ OCH₃ H O 0 A-1347 H H H H H CH₂CHF₂ OCH₃ H O 0 A-1348 H H H H H CH₂CClF₂ OCH₃ H O 0 A-1349 H H H H H CH₂CBrF₂ OCH₃ H O 0 A-1350 H H H H H CF₂CF₃ OCH₃ H O 0 A-1351 H H H H H CF₂CHF₂ OCH₃ H O 0 A-1352 H H H H H CH₂CH₂CF₃ OCH₃ H O 0 A-1353 H H H H H CH₂CF₂CF₃ OCH₃ H O 0 A-1354 H H H H H CH₂CF₂CHF₂ OCH₃ H O 0 A-1355 H H H H H CF₂CHFCF₃ OCH₃ H O 0 A-1356 H H H H H CF₂CF₂CF₃ OCH₃ H O 0 A-1357 H H H H H CH₂CF₂CF₂CF₃ OCH₃ H O 0 A-1358 H H H H H CH₂CF₂CHFCF₃ OCH₃ H O 0 A-1359 H H H H H CH₂CH₂CH₂CF₃ OCH₃ H O 0 A-1360 H H H H H CH₂CH₂CF₂CF₃ OCH₃ H O 0 A-1361 H H H H H CF₂CF₂CF₂CF₃ OCH₃ H O 0 A-1362 H H H H H CH₂CH₂CH(CF₃)₂ OCH₃ H O 0 A-1363 H H H H H CF₂CF₂CF₂CF₂CF₃ OCH₃ H O 0 A-1364 H H H H H CH₂CF₂CF₂CF₂CF₃ OCH₃ H O 0 A-1365 H H H H H CH₂CH₂CH₂CH₂CF₃ OCH₃ H O 0 A-1366 H H H H H CH₂CF₂CF₂CF₂CHF₂ OCH₃ H O 0 A-1367 H H H H H CH₂CH₂OCH₂CF₃ OCH₃ H O 0 A-1368 H H H H H CF₂CHFOCF₃ OCH₃ H O 0 A-1369 H H H H H CF₂CHFOCF₂CF₃ OCH₃ H O 0 A-1370 H H H H H CH₂CH₂CF═CF₂ OCH₃ H O 0 A-1371 H H H H H CH₂CH₂CH═CF₂ OCH₃ H O 0 A-1372 H H H H H CH₂C≡CCH₃ OCH₃ H O 0 A-1373 H H H H H CH₂C≡CCF₃ OCH₃ H O 0 A-1374 H H H H H CH₂C≡CI OCH₃ H O 0 A-1375 H H H H H CH₂(2,2-difluorocyclopropyl) OCH₃ H O 0 A-1376 H H H H H CH₂(2,2-dichlorocyclopropyl) OCH₃ H O 0 A-1377 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) OCH₃ H O 0 A-1378 H H H H H CH₂CH₂(2,2-(dichlorocyclopropyl) OCH₃ H O 0 A-1379 H H H H H CH₂SCH₃ OCH₃ H O 0 A-1380 H H H H H CH₂SCH₂CH₃ OCH₃ H O 0 A-1381 H H H H H CH₂CH₂SCH₃ OCH₃ H O 0 A-1382 H H H H H CH₂SOCH₃ OCH₃ H O 0 A-1383 H H H H H CH₂CH₂SOCH₃ OCH₃ H O 0 A-1384 H H H H H CH₂SO₂CH₃ OCH₃ H O 0 A-1385 H H H H H CH₂CH₂SO₂CH₃ OCH₃ H O 0 A-1386 H H H H H CH₂SCF₃ OCH₃ H O 0 A-1387 H H H H H CH₂SCHF₂ OCH₃ H O 0 A-1388 H H H H H CH₂SCH₂CF₃ OCH₃ H O 0 A-1389 H H H H H CH₂SCH₂CHF₂ OCH₃ H O 0 A-1390 H H H H H CH₂SCF₂CF₃ OCH₃ H O 0 A-1391 H H H H H CH₂CH₂SCF₃ OCH₃ H O 0 A-1392 H H H H H CH₂SOCF₃ OCH₃ H O 0 A-1393 H H H H H CH₂CH₂SOCF₃ OCH₃ H O 0 A-1394 H H H H H CH₂CH₂CH₂SOCF₃ OCH₃ H O 0 A-1395 H H H H H CH₂SO₂CF₃ OCH₃ H O 0 A-1396 H H H H H CH₂CH₂SO₂CF₃ OCH₃ H O 0 A-1397 H H H H H CH₂CH₂CH₂SO₂CF₃ OCH₃ H O 0 A-1398 H H H H H CH₂C(=O)NHCH₂CHF₂ OCH₃ H O 0

TABLE 24 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1399 H H H H H CH₂C(═O)NHCH₂CF₃ OCH₃ H O 0 A-1400 H H H H H H CH₂CF₃ H O 0 A-1401 H H H H H CH₃ CH₂CF₃ H O 0 A-1402 H H H H H CH₂CH₃ CH₂CF₃ H O 0 A-1403 H H H H H CH(CH3)₂ CH₂CF₃ H O 0 A-1404 H H H H H CH₂CH₂CH₃ CH₂CF₃ H O 0 A-1405 H H H H H CH₂CH(CH₃)₂ CH₂CF₃ H O 0 A-1406 H H H H H CH₂C(CH₃)₃ CH₂CF₃ H O 0 A-1407 H H H H H CH(CH3)CH₂CH₃ CH₂CF₃ H O 0 A-1408 H H H H H CH₂(CH₂)₂CH₃ CH₂CF₃ H O 0 A-1409 H H H H H CH₂(CH₂)₃CH₃ CH₂CF₃ H O 0 A-1410 H H H H H CH₂(CH₂)₄CH₃ CH₂CF₃ H O 0 A-1411 H H H H H CH₂(CH₂)₆CH₃ CH₂CF₃ H O 0 A-1412 H H H H H CH₂OCH₃ CH₂CF₃ H O 0 A-1413 H H H H H CH₂OCH₂CH₃ CH₂CF₃ H O 0 A-1414 H H H H H CH₂CH₂OCH₃ CH₂CF₃ H O 0 A-1415 H H H H H CH₂CH₂OCH₂CH₃ CH₂CF₃ H O 0 A-1416 H H H H H CF₃ CH₂CF₃ H O 0 A-1417 H H H H H CHF₂ CH₂CF₃ H O 0 A-1418 H H H H H CH₂CF₃ CH₂CF₃ H O 0 A-1419 H H H H H CH₂CHF₂ CH₂CF₃ H O 0 A-1420 H H H H H CH₂CClF₂ CH₂CF₃ H O 0 A-1421 H H H H H CH₂CBrF₂ CH₂CF₃ H O 0 A-1422 H H H H H CF₂CF₃ CH₂CF₃ H O 0 A-1423 H H H H H CF₂CHF₂ CH₂CF₃ H O 0 A-1424 H H H H H CH₂CH₂CF₃ CH₂CF₃ H O 0 A-1425 H H H H H CH₂CF₂CF₃ CH₂CF₃ H O 0 A-1426 H H H H H CH₂CF₂CHF₂ CH₂CF₃ H O 0 A-1427 H H H H H CF₂CHFCF₃ CH₂CF₃ H O 0 A-1428 H H H H H CF₂CF₂CF₃ CH₂CF₃ H O 0 A-1429 H H H H H CH₂CF₂CF₂CF₃ CH₂CF₃ H O 0 A-1430 H H H H H CH₂CF₂CHFCF₃ CH₂CF₃ H O 0 A-1431 H H H H H CH₂CH₂CH₂CF₃ CH₂CF₃ H O 0 A-1432 H H H H H CH₂CH₂CF₂CF₃ CH₂CF₃ H O 0 A-1433 H H H H H CF₂CF₂CF₂CF₃ CH₂CF₃ H O 0 A-1434 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CF₃ H O 0 A-1435 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CF₃ H O 0 A-1436 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CF₃ H O 0 A-1437 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CF₃ H O 0 A-1438 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CF₃ H O 0 A-1439 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CF₃ H O 0 A-1440 H H H H H CF₂CHFOCH₃ CH₂CF₃ H O 0 A-1441 H H H H H CF₂CHFOCH₂CH₃ CH₂CF₃ H O 0 A-1442 H H H H H CH₂CH₂OCH₂CF₃ CH₂CF₃ H O 0 A-1443 H H H H H CF₂CHFOCF₃ CH₂CF₃ H O 0 A-1444 H H H H H CF₂CHFOCF₂CF₃ CH₂CF₃ H O 0 A-1445 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₂CF₃ H O 0 A-1446 H H H H H CH₂CH═CH₂ CH₂CF₃ H O 0 A-1447 H H H H H CH₂CH═CHCl CH₂CF₃ H O 0 A-1448 H H H H H CH₂CH═CCl₂ CH₂CF₃ H O 0 A-1449 H H H H H CH₂CH₂CF═CF₂ CH₂CF₃ H O 0 A-1450 H H H H H CH₂CH₂CH═CF₂ CH₂CF₃ H O 0 A-1451 H H H H H CH₂CF≡CH CH₂CF₃ H O 0 A-1452 H H H H H CH₂C≡CCH₃ CH₂CF₃ H O 0 A-1453 H H H H H CH₂C≡CI CH₂CF₃ H O 0 A-1454 H H H H H CH₂C≡CCF₃ CH₂CF₃ H O 0 A-1455 H H H H H cyclobutyl CH₂CF₃ H O 0 A-1456 H H H H H cyclopentyl CH₂CF₃ H O 0 A-1457 H H H H H cyclohexyl CH₂CF₃ H O 0 A-1458 H H H H H 4,4-difluorocyclohexyl CH₂CF₃ H O 0 A-1459 H H H H H CH2(cyclopropyl) CH₂CF₃ H O 0

TABLE 25 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1460 H H H H H CH₂(cyclobutyl) CH₂CF₃ H O 0 A-1461 H H H H H CH₂(cyclopentyl) CH₂CF₃ H O 0 A-1462 H H H H H CH₂CH₂(cyclopropyl) CH₂CF₃ H O 0 A-1463 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CF₃ H O 0 A-1464 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CF₃ H O 0 A-1465 H H H H H CH₂(4,4-difluorocyclohexyl) CH₂CF₃ H O 0 A-1466 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CF₃ H O 0 A-1467 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CF₃ H O 0 A-1468 H H H H H CH₂SCH₃ CH₂CF₃ H O 0 A-1469 H H H H H CH₂SCH₂CH₃ CH₂CF₃ H O 0 A-1470 H H H H H CH₂CH₂SCH₃ CH₂CF₃ H O 0 A-1471 H H H H H CH₂CH₂SCH₂CH₃ CH₂CF₃ H O 0 A-1472 H H H H H CH₂CH₂CH₂SCH₃ CH₂CF₃ H O 0 A-1473 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CF₃ H O 0 A-1474 H H H H H CH(CH₃)SCH₃ CH₂CF₃ H O 0 A-1475 H H H H H CH(CH₃)SCH₂CH₃ CH₂CF₃ H O 0 A-1476 H H H H H CH₂CH(CH₃)SCH₃ CH₂CF₃ H O 0 A-1477 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CF₃ H O 0 A-1478 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₂CF₃ H O 0 A-1479 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CF₃ H O 0 A-1480 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CF₃ H O 0 A-1481 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CF₃ H O 0 A-1482 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CF₃ H O 0 A-1483 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₂ CH₂CF₃ H O 0 A-1484 H H H H H CH₂SOCH₃ CH₂CF₃ H O 0 A-1485 H H H H H CH₂CH₂SOCH₃ CH₂CF₃ H O 0 A-1486 H H H H H CH₂CH₂CH₂SOCH₃ CH₂CF₃ H O 0 A-1487 H H H H H CH(CH₃)SOCH₃ CH₂CF₃ H O 0 A-1488 H H H H H CH₂CH(CH₃)SOCH₃ CH₂CF₃ H O 0 A-1489 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CF₃ H O 0 A-1490 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CF₃ H O 0 A-1491 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CF₃ H O 0 A-1492 H H H H H CH₂SO₂CH₃ CH₂CF₃ H O 0 A-1493 H H H H H CH₂CH₂SO₂CH₃ CH₂CF₃ H O 0 A-1494 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₂CF₃ H O 0 A-1495 H H H H H CH(CH₃)SO₂CH₃ CH₂CF₃ H O 0 A-1496 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₂CF₃ H O 0 A-1497 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CF₃ H O 0 A-1498 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CF₃ H O 0 A-1499 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CF₃ H O 0 A-1500 H H H H H CH₂SCF₃ CH₂CF₃ H O 0 A-1501 H H H H H CH₂SCHF₂ CH₂CF₃ H O 0 A-1502 H H H H H CH₂SCH₂CF₃ CH₂CF₃ H O 0 A-1503 H H H H H CH₂SCH₂CHF₂ CH₂CF₃ H O 0 A-1504 H H H H H CH₂SCF₂CF₃ CH₂CF₃ H O 0 A-1505 H H H H H CH₂CH₂SCF₃ CH₂CF₃ H O 0 A-1506 H H H H H CH₂CH₂SCH₂CF₃ CH₂CF₃ H O 0 A-1507 H H H H H CH₂CH₂CH₂SCF₃ CH₂CF₃ H O 0 A-1508 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CF₃ H O 0 A-1509 H H H H H CH(CH₃)SCF₃ CH₂CF₃ H O 0 A-1510 H H H H H CH(CH₃)SCH₂CF₃ CH₂CF₃ H O 0 A-1511 H H H H H CH₂CH(CH₃)SCF₃ CH₂CF₃ H O 0 A-1512 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CF₃ H O 0 A-1513 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CF₃ H O 0 A-1514 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CF₃ H O 0 A-1515 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CF₃ H O 0 A-1516 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CF₃ H O 0 A-1517 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₂CF₃ H O 0 A-1518 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CF₃ H O 0 A-1519 H H H H H CH₂SOCF₃ CH₂CF₃ H O 0 A-1520 H H H H H CH₂CH₂SOCF₃ CH₂CF₃ H O 0

TABLE 26 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1521 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CF₃ H O 0 A-1522 H H H H H CH(CH₃)SOCF₃ CH₂CF₃ H O 0 A-1523 H H H H H CH₂CH(CH₃)SOCF₃ CH₂CF₃ H O 0 A-1524 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CF₃ H O 0 A-1525 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CF₃ H O 0 A-1526 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CF₃ H O 0 A-1527 H H H H H CH₂SO₂CF₃ CH₂CF₃ H O 0 A-1528 H H H H H CH₂CH₂SO₂CF₃ CH₂CF₃ H O 0 A-1529 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CF₃ H O 0 A-1530 H H H H H CH(CH₃)SO₂CF₃ CH₂CF₃ H O 0 A-1531 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₂CF₃ H O 0 A-1532 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CF₃ H O 0 A-1533 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CF₃ H O 0 A-1534 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CF₃ H O 0 A-1535 H H H H H CH₂C(═O)CH₃ CH₂CF₃ H O 0 A-1536 H H H H H CH₂C(═O)CH₂CH₃ CH₂CF₃ H O 0 A-1537 H H H H H CH₂C(═O)C(CH₃)₃ CH₂CF₃ H O 0 A-1538 H H H H H CH₂CH₂C(═O)CH₃ CH₂CF₃ H O 0 A-1539 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CF₃ H O 0 A-1540 H H H H H CH₂C(═O)CF₃ CH₂CF₃ H O 0 A-1541 H H H H H CH₂CH₂C(═O)CF₃ CH₂CF₃ H O 0 A-1542 H H H H H CH₂C(═O)OCH₃ CH₂CF₃ H O 0 A-1543 H H H H H CH₂C(═O)OCH₂CH₃ CH₂CF₃ H O 0 A-1544 H H H H H CH₂C(═O)OC(CH₃)₃ CH₂CF₃ H O 0 A-1545 H H H H H CH₂CH₂C(═O)OCH₃ CH₂CF₃ H O 0 A-1546 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CF₃ H O 0 A-1547 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CF₃ H O 0 A-1548 H H H H H CH₂C(═O)NH₂ CH₂CF₃ H O 0 A-1549 H H H H H CH₂CH₂C(═O)NH₂ CH₂CF₃ H O 0 A-1550 H H H H H CH₂C(═O)NHCH₃ CH₂CF₃ H O 0 A-1551 H H H H H CH₂C(H═O)NHCH(CH₃)₂ CH₂CF₃ H O 0 A-1552 H H H H H CH₂CH₂C(═O)NHCH₃ CH₂CF₃ H O 0 A-1553 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CF₃ H O 0 A-1554 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CF₃ H O 0 A-1555 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CF₃ H O 0 A-1556 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CF₃ H O 0 A-1557 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CF₃ H O 0 A-1558 H H H H H CH₂C(═O)N(CH₃)₂ CH₂CF₃ H O 0 A-1559 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CF₃ H O 0 A-1560 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CF₃ H O 0 A-1561 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CF₃ H O 0 A-1562 H H H H H CH₂CH₂OH CH₂CF₃ H O 0 A-1563 H H H H H CH₂CH(OH)CH₃ CH₂CF₃ H O 0 A-1564 H H H H H CH₂CH₂CH₂OH CH₂CF₃ H O 0 A-1565 H H H H H CH₂CH(OH)CH₂CH₃ CH₂CF₃ H O 0 A-1566 H H H H H CH₂CH(OH)C(CH₃)₃ CH₂CF₃ H O 0 A-1567 H H H H H CH₂CH₂CH(OH)CH₃ CH₂CF₃ H O 0 A-1568 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CF₃ H O 0 A-1569 H H H H H CH₂C(═NOH)CH₃ CH₂CF₃ H O 0 A-1570 H H H H H CH₂C(═NOH)CH₂CH₃ CH₂CF₃ H O 0 A-1571 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₂CF₃ H O 0 A-1572 H H H H H CH₂C(═NOCH₃)CH₃ CH₂CF₃ H O 0 A-1573 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CF₃ H O 0 A-1574 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CF₃ H O 0 A-1575 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CF₃ H O 0 A-1576 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CF₃ H O 0 A-1577 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CF₃ H O 0 A-1578 H H H H H CH₂Ph CH₂CF₃ H O 0 A-1579 H H H H H CH₂(2-F)Ph CH₂CF₃ H O 0 A-1580 H H H H H CH₂(3-F)Ph CH₂CF₃ H O 0 A-1581 H H H H H CH₂(4-F)Ph CH₂CF₃ H O 0

TABLE 27 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1582 H H H H H CH₂(2-Cl)Ph CH₂CF₃ H O 0 A-1583 H H H H H CH₂(3-Cl)Ph CH₂CF₃ H O 0 A-1584 H H H H H CH₂(4-Cl)Ph CH₂CF₃ H O 0 A-1585 H H H H H CH₂(2-CF₃)Ph CH₂CF₃ H O 0 A-1586 H H H H H CH₂(3-CF₃)Ph CH₂CF₃ H O 0 A-1587 H H H H H CH₂(4-CF₃)Ph CH₂CF₃ H O 0 A-1588 H H H H H CH₂(naphthalen-1-yl) CH₂CF₃ H O 0 A-1589 H H H H H CH₂(naphthalen-2-yl) CH₂CF₃ H O 0 A-1590 H H H H H CH₂CH₂Ph CH₂CF₃ H O 0 A-1591 H H H H H H 4-tetrahydropyranyl H O 0 A-1592 H H H H H CH₃ 4-tetrahydropyranyl H O 0 A-1593 H H H H H CH₂CH₃ 4-tetrahydropyranyl H O 0 A-1594 H H H H H CH(CH₃)₂ 4-tetrahydropyranyl H O 0 A-1595 H H H H H CH₂CH₂CH₃ 4-tetrahydropyranyl H O 0 A-1596 H H H H H CH₂CH(CH₃)₂ 4-tetrahydropyranyl H O 0 A-1597 H H H H H CH(CH₃)CH₂CH₃ 4-tetrahydropyranyl H O 0 A-1598 H H H H H CH₂C(CH₃)₃ 4-tetrahydropyranyl H O 0 A-1599 H H H H H CH₂(CH₂)₂CH₃ 4-tetrahydropyranyl H O 0 A-1600 H H H H H CH₂(CH₂)₃CH₃ 4-tetrahydropyranyl H O 0 A-1601 H H H H H CF₃ 4-tetrahydropyranyl H O 0 A-1602 H H H H H CHF₂ 4-tetrahydropyranyl H O 0 A-1603 H H H H H CH₂CF₃ 4-tetrahydropyranyl H O 0 A-1604 H H H H H CH₂CHF₂ 4-tetrahydropyranyl H O 0 A-1605 H H H H H CH₂CClF₂ 4-tetrahydropyranyl H O 0 A-1606 H H H H H CH₂CBrF₂ 4-tetrahydropyranyl H O 0 A-1607 H H H H H CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1608 H H H H H CF₂CHF₂ 4-tetrahydropyranyl H O 0 A-1609 H H H H H CH₂CH₂CF₃ 4-tetrahydropyranyl H O 0 A-1610 H H H H H CH₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1611 H H H H H CH₂CF₂CHF₂ 4-tetrahydropyranyl H O 0 A-1612 H H H H H CF₂CHFCF₃ 4-tetrahydropyranyl H O 0 A-1613 H H H H H CF₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1614 H H H H H CH₂CF₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1615 H H H H H CH₂CF₂CHFCF₃ 4-tetrahydropyrany1 H O 0 A-1616 H H H H H CH₂CH₂CH₂CF₃ 4-tetrahydropyranyl H O 0 A-1617 H H H H H CH₂CH₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1618 H H H H H CF₂CF₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1619 H H H H H CH₂CH₂CH(CF₃)₂ 4-tetrahydropyranyl H O 0 A-1620 H H H H H CF₂CF₂CF₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1621 H H H H H CH₂CF₂CF₂CF₂CF₃ 4-tetrahydropyranyl H O 0 A-1622 H H H H H CH₂CH₂CH₂CH₂CF₃ 4-tetrahydropyranyl H O 0 A-1623 H H H H H CH₂CF₂CF₂CF₂CHF₂ 4-tetrahydropyranyl H O 0 A-1624 H H H H H CH₂CH₂OCH₂CF₃ 4-tetrahydropyranyl H O 0 A-1625 H H H H H CF₂CHFOCF₃ 4-tetrahydropyranyl H O 0 A-1626 H H H H H CF₂CHFOCF₂CF₃ 4-tetrahydropyranyl H O 0 A-1627 H H H H H CH₂CH₂CF═CF₂ 4-tetrahydropyranyl H O 0 A-1628 H H H H H CH₂CH₂CH═CF₂ 4-tetrahydropyranyl H O 0 A-1629 H H H H H CH₂C≡CCH₃ 4-tetrahydropyranyl H O 0 A-1630 H H H H H CH₂C≡CCF₃ 4-tetrahydropyranyl H O 0 A-1631 H H H H H CH₂C═CL 4-tetrahydropyranyl H O 0 A-1632 H H H H H CH₂(2,2-difluorocyclopropyl) 4-tetrahydropyranyl H O 0 A-1633 H H H H H CH₂(2,2-dichlorocyclopropyl) 4-tetrahydropyranyl H O 0 A-1634 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) 4-tetrahydropyranyl H O 0 A-1635 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) 4-tetrahydropyranyl H O 0 A-1636 H H H H H CH₂SCH₃ 4-tetrahydropyranyl H O 0 A-1637 H H H H H CH₂SCH₂CH₃ 4-tetrahydropyranyl H O 0 A-1638 H H H H H CH₂CH₂SCH₃ 4-tetrahydropyranyl H O 0 A-1639 H H H H H CH₂SOCH₃ 4-tetrahydropyranyl H O 0 A-1640 H H H H H CH₂CH₂SOCH₃ 4-tetrahydropyranyl H O 0 A-1641 H H H H H CH₂CH₂SO₂CH₃ 4-tetrahydropyranyl H O 0 A-1642 H H H H H CH₂CH₂SO₂CH₃ 4-tetrahydropyranyl H O 0

TABLE 28 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1643 H H H H H CH₂SCF₃ 4-tetrahydropyranyl H O 0 A-1644 H H H H H CH₂SCHF₂ 4-tetrahydropyranyl H O 0 A-1645 H H H H H CH₂SCH₂CF₃ 4-tetrahydropyranyl H O 0 A-1646 H H H H H CH₂SCH₂CHF₂ 4-tetrahydropyranyl H O 0 A-1647 H H H H H CH₂SCF₂CF₂ 4-tetrahydropyranyl H O 0 A-1648 H H H H H CH₂CH₂SCF₃ 4-tetrahydropyranyl H O 0 A-1649 H H H H H CH₂SOCF₃ 4-tetrahydropyranyl H O 0 A-1650 H H H H H CH₂CH₂SOCF₃ 4-tetrahydropyranyl H O 0 A-1651 H H H H H CH₂CH₂CH₂SOCF₃ 4-tetrahydropyranyl H O 0 A-1652 H H H H H CH₂SO₂CF₃ 4-tetrahydropyranyl H O 0 A-1653 H H H H H CH₂CH₂SO₂CF₃ 4-tetrahydropyranyl H O 0 A-1654 H H H H H CH₂CH₂CH₂SO₂CF₃ 4-tetrahydropyranyl H O 0 A-1655 H H H H H CH₂C(═O)NHCH₂CHF₂ 4-tetrahydropyranyl H O 0 A-1656 H H H H H CH₂C(═O)NHCH₂CF₃ 4-tetrahydropyranyl H O 0 A-1657 H H H H H H CH₂CN H O 0 A-1658 H H H H H CH₃ CH₂CN H O 0 A-1659 H H H H H CH₂CH₃ CH₂CN H O 0 A-1660 H H H H H CH(CH₃)₂ CH₂CN H O 0 A-1661 H H H H H CH₂CH₂CH₃ CH₂CN H O 0 A-1662 H H H H H CH₂CH(CH₃)₂ CH₂CN H O 0 A-1663 H H H H H CH(CH₃)CH₂CH₃ CH₂CN H O 0 A-1664 H H H H H CH₂C(CH₃)₃ CH₂CN H O 0 A-1665 H H H H H CH₂(CH₂)₂CH₃ CH₂CN H O 0 A-1666 H H H H H CH₂(CH₂)₃CH₃ CH₂CN H O 0 A-1667 H H H H H CH₂(CH₂)₄CH₃ CH₂CN H O 0 A-1668 H H H H H CH₂(CH₂)₆CH₃ CH₂CN H O 0 A-1669 H H H H H CH₂OCH₃ CH₂CN H O 0 A-1670 H H H H H CH₂OCH₂CH₃ CH₂CN H O 0 A-1671 H H H H H CH₂CH₂OCH₃ CH₂CN H O 0 A-1672 H H H H H CH₂CH₂OCH₂CH₃ CH₂CN H O 0 A-1673 H H H H H CF₃ CH₂CN H O 0 A-1674 H H H H H CHF₂ CH₂CN H O 0 A-1675 H H H H H CH₂CF₃ CH₂CN H O 0 A-1676 H H H H H CH₂CHF₂ CH₂CN H O 0 A-1677 H H H H H CH₂CClF₂ CH₂CN H O 0 A-1678 H H H H H CH₂CBrF₂ CH₂CN H O 0 A-1679 H H H H H CF₂CF₃ CH₂CN H O 0 A-1680 H H H H H CF₂CHF₂ CH₂CN H O 0 A-1681 H H H H H CH₂CH₂CF₃ CH₂CN H O 0 A-1682 H H H H H CH₂CF₂CF₃ CH₂CN H O 0 A-1683 H H H H H CH₂CF₂CHF₂ CH₂CN H O 0 A-1684 H H H H H CF₂CHFCF₃ CH₂CN H O 0 A-1685 H H H H H CF₂CF₂CF₃ CH₂CN H O 0 A-1686 H H H H H CH₂CF₂CF₂CF₃ CH₂CN H O 0 A-1687 H H H H H CH₂CF₂CHFCF₃ CH₂CN H O 0 A-1688 H H H H H CH₂CH₂CH₂CF₃ CH₂CN H O 0 A-1689 H H H H H CH₂CH₂CF₂CF₃ CH₂CN H O 0 A-1690 H H H H H CF₂CF₂CF₂CF₃ CH₂CN H O 0 A-1691 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CN H O 0 A-1692 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CN H O 0 A-1693 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CN H O 0 A-1694 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CN H O 0 A-1695 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CN H O 0 A-1696 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CN H O 0 A-1697 H H H H H CF₂CHFOCH₃ CH₂CN H O 0 A-1698 H H H H H CF₂CHFOCH₂CH₃ CH₂CN H O 0 A-1699 H H H H H CH₂CH₂OCH₂CF₃ CH₂CN H O 0 A-1700 H H H H H CF₂CHFOCF₃ CH₂CN H O 0 A-1701 H H H H H CF₂CHFOCF₂CF₃ CH₂CN H O 0 A-1702 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₂CN H O 0 A-1703 H H H H H CH₂CH═CH₂ CH₂CN H O 0

TABLE 29 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1704 H H H H H CH₂CH═CHCl CH₂CN H O 0 A-1705 H H H H H CH₂CH═CCl₂ CH₂CN H O 0 A-1706 H H H H H CH₂CH₂CF═CF₂ CH₂CN H O 0 A-1707 H H H H H CH₂CH₂CH═CF₂ CH₂CN H O 0 A-1708 H H H H H CH₂C≡CH CH₂CN H O 0 A-1709 H H H H H CH₂C≡CCH₃ CH₂CN H O 0 A-1710 H H H H H CH₂C≡CCF₃ CH₂CN H O 0 A-1711 H H H H H CH₂C≡CI CH₂CN H O 0 A-1712 H H H H H cyclobutyl CH₂CN H O 0 A-1713 H H H H H cyclopentyl CH₂CN H O 0 A-1711 H H H H H cyclohexyl CH₂CN H O 0 A-1715 H H H H H 4,4-difluorocyclohexyl CH₂CN H O 0 A-1716 H H H H H CH₂(cyclopropyl) CH₂CN H O 0 A-1717 H H H H H CH₂(cyclobutyl) CH₂CN H O 0 A-1718 H H H H H CH₂(cyclopentyl) CH₂CN H O 0 A-1719 H H H H H CH₂CH₂(cyclopropyl) CH₂CN H O 0 A-1720 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CN H O 0 A-1721 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CN H O 0 A-1722 H H H H H CH₂(4,4-difluorocyclohexyl) CH₂CN H O 0 A-1723 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CN H O 0 A-1724 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CN H O 0 A-1725 H H H H H CH₂SCH₃ CH₂CN H O 0 A-1725 H H H H H CH₂SCH₂CH₃ CH₂CN H O 0 A-1727 H H H H H CH₂CH₂SCH₃ CH₂CN H O 0 A-1726 H H H H H CH₂CH₂SCH₂CH₃ CH₂CN H O 0 A-1729 H H H H H CH₂CH₂CH₂SCH₃ CH₂CN H O 0 A-1730 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CN H O 0 A-1731 H H H H H CH(CH₃)SCH₃ CH₂CN H O 0 A-1732 H H H H H CH(CH₃)SCH₂CH₃ CH₂CN H O 0 A-1733 H H H H H CH₂CH(CH₃)SCH₃ CH₂CN H O 0 A-1734 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CN H O 0 A-1735 H H H H H CH(CH₃)CH₂CH₂SCH₂ CH₂CN H O 0 A-1736 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CN H O 0 A-1737 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CN H O 0 A-1738 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CN H O 0 A-1739 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CN H O 0 A-1740 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CN H O 0 A-1741 H H H H H CH₂SOCH₃ CH₂CN H O 0 A-1742 H H H H H CH₂CH₂SOCH₃ CH₂CN H O 0 A-1743 H H H H H CH₂CH₂CH₂SOCH₃ CH₂CN H O 0 A-1744 H H H H H CH(CH₃)SOCH₃ CH₂CN H O 0 A-1745 H H H H H CH₂CH(CH₃)SOCH₃ CH₂CN H O 0 A-1746 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CN H O 0 A-1747 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CN H O 0 A-1748 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CN H O 0 A-1749 H H H H H CH₂SO₂CH₃ CH₂CN H O 0 A-1750 H H H H H CH₂CH₂SO₂CH₃ CH₂CN H O 0 A-1751 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₂CN H O 0 A-1752 H H H H H CH(CH₃)SO₂CH₃ CH₂CN H O 0 A-1753 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₂CN H O 0 A-1754 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CN H O 0 A-1755 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CN H O 0 A-1756 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CN H O 0 A-1757 H H H H H CH₂SCF₃ CH₂CN H O 0 A-1758 H H H H H CH₂SCHF₂ CH₂CN H O 0 A-1759 H H H H H CH₂SCH₂CF₃ CH₂CN H O 0 A-1760 H H H H H CH₂SCH₂CHF₂ CH₂CN H O 0 A-1761 H H H H H CH₂SCF₂CF₃ CH₂CN H O 0 A-1762 H H H H H CH₂CH₂SCF₃ CH₂CN H O 0 A-1763 H H H H H CH₂CH₂SCH₂CF₃ CH₂CN H O 0 A-1764 H H H H H CH₂CH₂CH₂SCF₃ CH₂CN H O 0

TABLE 30 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1765 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CN H O 0 A-1766 H H H H H CH(CH₃)SCF₃ CH₂CN H O 0 A-1767 H H H H H CH(CH₃)SCH₂CF₃ CH₂CN H O 0 A-1768 H H H H H CH₂CH(CH₃)SCF₃ CH₂CN H O 0 A-1769 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CN H O 0 A-1770 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CN H O 0 A-1771 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CN H O 0 A-1772 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CN H O 0 A-1773 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CN H O 0 A-1774 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₂CN H O 0 A-1775 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CN H O 0 A-1776 H H H H H CH₂SOCF₃ CH₂CN H O 0 A-1777 H H H H H CH₂CH₂SOCF₃ CH₂CN H O 0 A-1778 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CN H O 0 A-1779 H H H H H CH(CH₃)SOCF₃ CH₂CN H O 0 A-1780 H H H H H CH₂CH(CH₃)SOCF₃ CH₂CN H O 0 A-1781 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CN H O 0 A-1782 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CN H O 0 A-1783 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CN H O 0 A-1784 H H H H H CH₂SO₂CF₃ CH₂CN H O 0 A-1785 H H H H H CH₂CH₂SO₂CF₃ CH₂CN H O 0 A-1786 H H H H H CH₂CH₂CH₂SO₂CF₂ CH₂CN H O 0 A-1787 H H H H H CH(CH₃)SO₂CF₃ CH₂CN H O 0 A-1788 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₂CN H O 0 A-1789 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CN H O 0 A-1790 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CN H O 0 A-1791 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CN H O 0 A-1792 H H H H H CH₂C(═O)CH₃ CH₂CN H O 0 A-1793 H H H H H CH₂C(═O)CH₂CH₃ CH₂CN H O 0 A-1794 H H H H H CH₂C(═O)C(OH₃)₃ CH₂CN H O 0 A-1795 H H H H H CH₂CH₂C(═O)CH₃ CH₂CN H O 0 A-1796 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CN H O 0 A-1797 H H H H H CH₂C(═O)CF₃ CH₂CN H O 0 A-1798 H H H H H CH₂CH₂C(═O)CF₃ CH₂CN H O 0 A-1799 H H H H H CH₂C(═O)OCH₃ CH₂CN H O 0 A-1800 H H H H H CH₂C(═O)OCH₂CH₃ CH₂CN H O 0 A-1801 H H H H H CH₂C(═O)OC(CH₃)₃ CH₂CN H O 0 A-1802 H H H H H CH₂CH₂C(═O)OCH₃ CH₂CN H O 0 A-1803 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CN H O 0 A-1804 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CN H O 0 A-1805 H H H H H CH₂C(═O)NH₂ CH₂CN H O 0 A-1806 H H H H H CH₂CH₂C(═O)NH₂ CH₂CN H O 0 A-1807 H H H H H CH₂C(═O)NHCH₃ CH₂CN H O 0 A-1808 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₂CN H O 0 A-1809 H H H H H CH₂CH₂C(═O)NHCH₃ CH₂CN H O 0 A-1810 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CN H O 0 A-1811 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CN H O 0 A-1812 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CN H O 0 A-1813 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CN H O 0 A-1814 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CN H O 0 A-1815 H H H H H CH₂C(═O)N(CH₃)₂ CH₂CN H O 0 A-1816 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CN H O 0 A-1817 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CN H O 0 A-1818 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CN H O 0 A-1819 H H H H H CH₂CH₂OH CH₂CN H O 0 A-1820 H H H H H CH₂CH(OH)CH₃ CH₂CN H O 0 A-1821 H H H H H CH₂CH₂CH₂OH CH₂CN H O 0 A-1822 H H H H H CH₂CH(OH)CH₂CH₃ CH₂CN H O 0 A-1823 H H H H H CH₂CH(OH)C(CH₃)₃ CH₂CN H O 0 A-1824 H H H H H CH₂CH₂CH(OH)CH₃ CH₂CN H O 0 A-1825 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CN H O 0

TABLE 31 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1826 H H H H H CH₂C(═NOH)CH₃ CH₂CN H O 0 A-1827 H H H H H CH₂C(═NOH)CH₂CH₃ CH₂CN H O 0 A-1828 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₂CN H O 0 A-1829 H H H H H CH₂C(═NOCH₃)CH₃ CH₂CN H O 0 A-1830 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CN H O 0 A-1831 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CN H O 0 A-1832 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CN H O 0 A-1833 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CN H O 0 A-1834 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₂ CH₂CN H O 0 A-1835 H H H H H CH₂Ph CH₂CN H O 0 A-1836 H H H H H CH₂(2-F)Ph CH₂CN H O 0 A-1837 H H H H H CH₂(3-F)Ph CH₂CN H O 0 A-1838 H H H H H CH₂(4-F)Ph CH₂CN H O 0 A-1839 H H H H H CH₂(2-Cl)Ph CH₂CN H O 0 A-1840 H H H H H CH₂(3-Cl)Ph CH₂CN H O 0 A-1841 H H H H H CH₂(4-Cl)Ph CH₂CN H O 0 A-1842 H H H H H CH₂(2-CF₃)Ph CH₂CN H O 0 A-1843 H H H H H CH₂(3-CF₃)Ph CH₂CN H O 0 A-1844 H H H H H CH₂(4-CF₃)Ph CH₂CN H O 0 A-1845 H H H H H CH₂(naphthalen-1-yl) CH₂CN H O 0 A-1846 H H H H H CH₂(naphthalen-2-yl) CH₂CN H O 0 A-1847 H H H H H CH₂CH₂Ph CH₂CN H O 0 A-1848 H H H H H H CH₂CH₂CN H O 0 A-1849 H H H H H CH₃ CH₂CH₂CN H O 0 A-1850 H H H H H CH₂CH₃ CH₂CH₂CN H O 0 A-1851 H H H H H CH(CH₃)₂ CH₂CH₂CN H O 0 A-1852 H H H H H CH₂CH₂CH₃ CH₂CH₂CN H O 0 A-1853 H H H H H CH₂CH(CH₃)₂ CH₂CH₂CN H O 0 A-1854 H H H H H CH(CH₃)CH₂CH₃ CH₂CH₂CN H O 0 A-1855 H H H H H CH₂C(CH₃)₃ CH₂CH₂CN H O 0 A-1856 H H H H H CH₂(CH₂)₂CH₃ CH₂CH₂CN H O 0 A-1857 H H H H H CH₂(CH₂)₃CH₃ CH₂CH₂CN H O 0 A-1858 H H H H H CF₃ CH₂CH₂CN H O 0 A-1859 H H H H H CHF₂ CH₂CH₂CN H O 0 A-1860 H H H H H CH₂CF₃ CH₂CH₂CN H O 0 A-1861 H H H H H CH₂CHF₂ CH₂CH₂CN H O 0 A-1862 H H H H H CH₂CClF₂ CH₂CH₂CN H O 0 A-1863 H H H H H CH₂CBrF₂ CH₂CH₂CN H O 0 A-1864 H H H H H CF₂CF₃ CH₂CH₂CN H O 0 A-1865 H H H H H CF₂CHF₂ CH₂CH₂CN H O 0 A-1866 H H H H H CH₂CH₂CF₃ CH₂CH₂CN H O 0 A-1867 H H H H H CH₂CF₂CF₃ CH₂CH₂CN H O 0 A-1868 H H H H H CH₂CF₂CHF₂ CH₂CH₂CN H O 0 A-1869 H H H H H CF₂CHFCF₃ CH₂CH₂CN H O 0 A-1870 H H H H H CF₂CF₂CF₃ CH₂CH₂CN H O 0 A-1871 H H H H H CH₂CF₂CF₂CF₃ CH₂CH₂CN H O 0 A-1872 H H H H H CH₂CF₂CHFCF₃ CH₂CH₂CN H O 0 A-1873 H H H H H CH₂CH₂CH₂CF₃ CH₂CH₂CN H O 0 A-1874 H H H H H CH₂CH₂CF₂CF₃ CH₂CH₂CN H O 0 A-1875 H H H H H CF₂CF₂CF₂CF₃ CH₂CH₂CN H O 0 A-1876 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CH₂CN H O 0 A-1877 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₂CN H O 0 A-1878 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₂CN H O 0 A-1879 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₂CN H O 0 A-1880 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₂CN H O 0 A-1881 H H H H H CH₂CH₂OCH₂CF₃ CH₂CH₂CN H O 0 A-1882 H H H H H CF₂CHFOCF₃ CH₂CH₂CN H O 0 A-1883 H H H H H CF₂CHFOCF₂CF₃ CH₂CH₂CN H O 0 A-1884 H H H H H CH₂CH₂CF═CF₂ CH₂CH₂CN H O 0 A-1885 H H H H H CH₂CH₂CH═CF₂ CH₂CH₂CN H O 0 A-1886 H H H H H CH₂C≡CCH₃ CH₂CH₂CN H O 0

TABLE 32 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1887 H H H H H CH₂C≡CCF₃ CH₂CH₂CN H O 0 A-1888 H H H H H CH₂C≡CI CH₂CH₂CN H O 0 A-1889 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₂CN H O 0 A-1890 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₂CN H O 0 A-1891 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₂CN H O 0 A-1892 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₂CN H O 0 A-1893 H H H H H CH₂SCH₃ CH₂CH₂CN H O 0 A-1894 H H H H H CH₂SCH₂CH₃ CH₂CH₂CN H O 0 A-1895 H H H H H CH₂CH₂SCH CH₂CH₂CN H O 0 A-1896 H H H H H CH₂SOCH₃ CH₂CH₂CN H O 0 A-1897 H H H H H CH₂CH₂SOCH₃ CH₂CH₂CN H O 0 A-1898 H H H H H CH₂SO₂CH₃ CH₂CH₂CN H O 0 A-1899 H H H H H CH₂CH₂SO₂CH₃ CH₂CH₂CN H O 0 A-1900 H H H H H CH₂SCF₃ CH₂CH₂CN H O 0 A-1901 H H H H H CH₂SCHF₂ CH₂CH₂CN H O 0 A-1902 H H H H H CH₂SCH₂CF₃ CH₂CH₂CN H O 0 A-1903 H H H H H CH₂SCH₂CHF₂ CH₂CH₂CN H O 0 A-1904 H H H H H CH₂SCF₂CF₃ CH₂CH₂CN H O 0 A-1905 H H H H H CH₂CH₂SCF₃ CH₂CH₂CN H O 0 A-1906 H H H H H CH₂SOCF₃ CH₂CH₂CN H O 0 A-1907 H H H H H CH₂CH₂SOCF₃ CH₂CH₂CN H O 0 A-1908 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CH₂CN H O 0 A-1909 H H H H H CH₂SO₂CF₃ CH₂CH₂CN H O 0 A-1910 H H H H H CH₂CH₂SO₂CF₃ CH₂CH₂CN H O 0 A-1911 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₂CN H O 0 A-1912 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₂CN H O 0 A-1913 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₂CN H O 0 A-1914 H H H H H H 1-CN-cyclopropyl H O 0 A-1915 H H H H H CH₃ 1-CN-cyclopropyl H O 0 A-1916 H H H H H CH₂CH₃ 1-CN-cyclopropyl H O 0 A-1917 H H H H H CH(CH₃)₂ 1-CN-cyclopropyl H O 0 A-1918 H H H H H CH₂CH₂CH₃ 1-CN-cyclopropyl H O 0 A-1919 H H H H H CH₂CH(CH₃)₂ 1-CN-cyclopropyl H O 0 A-1920 H H H H H CH(CH₃)CH₂CH₃ 1-CN-cyclopropyl H O 0 A-1921 H H H H H CH₂C(CH₃)₃ 1-CN-cyclopropyl H O 0 A-1922 H H H H H CH₂(CH₂)₂CH₃ 1-CN-cyclopropyl H O 0 A-1923 H H H H H CH₂(CH₂)₃CH₃ 1-CN-cyclopropyl H O 0 A-1924 H H H H H CF₃ 1-CN-cyclopropyl H O 0 A-1925 H H H H H CHF₂ 1-CN-cyclopropyl H O 0 A-1926 H H H H H CH₂CF₃ 1-CN-cyclopropyl H O 0 A-1927 H H H H H CH₂CHF₂ 1-CN-cyclopropyl H O 0 A-1928 H H H H H CH₂CClF₂ 1-CN-cyclopropyl H O 0 A-1929 H H H H H CH₂CBrF₂ 1-CN-cyclopropyl H O 0 A-1930 H H H H H CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1931 H H H H H CF₂CHF₂ 1-CN-cyclopropyl H O 0 A-1932 H H H H H CH₂CH₂CF₃ 1-CN-cyclopropyl H O 0 A-1933 H H H H H CH₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1934 H H H H H CH₂CF₂CHF₂ 1-CN-cyclopropyl H O 0 A-1935 H H H H H CF₂CHFCF₃ 1-CN-cyclopropyl H O 0 A-1936 H H H H H CF₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1937 H H H H H CH₂CF₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1938 H H H H H CH₂CF₃CHFCF₃ 1-CN-cyclopropyl H O 0 A-1939 H H H H H CH₂CH₂CH₂CF₃ 1-CN-cyclopropyl H O 0 A-1940 H H H H H CH₂CH₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1941 H H H H H CF₂CF₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1942 H H H H H CH₂CH₂CH(CF₃)₂ 1-CN-cyclopropyl H O 0 A-1943 H H H H H CF₂CF₂CF₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1944 H H H H H CH₂CF₂CF₂CF₂CF₃ 1-CN-cyclopropyl H O 0 A-1945 H H H H H CH₂CH₂CH₂CH₂CF₃ 1-CN-cyclopropyl H O 0 A-1946 H H H H H CH₂CF₂CF₂CF₂CHF₂ 1-CN-cyclopropyl H O 0 A-1947 H H H H H CF₂CH₂OCH₂CF₃ 1-CN-cyclopropyl H O 0

TABLE 33 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-1948 H H H H H CF₂CHFOCF₃ 1-CN-cyclopropyl H O 0 A-1949 H H H H H CF₂CHFOCF₂CF₃ 1-CN-cyclopropyl H O 0 A-1950 H H H H H CH₂CH₂CF═CF₂ 1-CN-cyclopropyl H O 0 A-1951 H H H H H CH₂CH₂CH═CF₂ 1-CN-cyclopropyl H O 0 A-1952 H H H H H CH₂C≡CCH₃ 1-CN-cyclopropyl H O 0 A-1953 H H H H H CH₂C≡CCF₃ 1-CN-cyclopropyl H O 0 A-1954 H H H H H CH₂C≡CI 1-CN-cyclopropyl H O 0 A-1955 H H H H H CH₂(2,2-difluorocyclopropyl) 1-CN-cyclopropyl H O 0 A-1956 H H H H H CH₂(2,2-dichlorocyclopropyl) 1-CN-cyclopropyl H O 0 A-1957 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) 1-CN-cyclopropyl H O 0 A-1958 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) 1-CN-cyclopropyl H O 0 A-1959 H H H H H CH₂SCH₃ 1-CN-cyclopropyl H O 0 A-1960 H H H H H CH₂SCH₂CH₃ 1-CN-cyclopropyl H O 0 A-1961 H H H H H CH₂CH₂SCH₃ 1-CN-cyclopropyl H O 0 A-1962 H H H H H CH₂SOCH₃ 1-CN-cyclopropyl H O 0 A-1963 H H H H H CH₂CH₂SOCH₃ 1-CN-cyclopropyl H O 0 A-1964 H H H H H CH₂SO₂CH₂ 1-CN-cyclopropyl H O 0 A-1965 H H H H H CH₂CH₂SO₂CH₃ 1-CN-cyclopropyl H O 0 A-1966 H H H H H CH₂SCF₃ 1-CN-cyclopropyl H O 0 A-1967 H H H H H CH₂SCHF₂ 1-CN-cyclopropyl H O 0 A-1968 H H H H H CH₂SCH₂CF₃ 1-CN-cyclopropyl H O 0 A-1969 H H H H H CH₂SCH₂CHF₂ 1-CN-cyclopropyl H O 0 A-1970 H H H H H CH₂SCF₂CF₃ 1-CN-cyclopropyl H O 0 A-1971 H H H H H CH₂CH₂SCF₃ 1-CN-cyclopropyl H O 0 A-1972 H H H H H CH₂SOCF₃ 1-CN-cyclopropyl H O 0 A-1973 H H H H H CH₂CH₂SOCF₃ 1-CN-cyclopropyl H O 0 A-1974 H H H H H CH₂CH₂CH₂SOCF₃ 1-CN-cyclopropyl H O 0 A-1975 H H H H H CH₂SO₂CF₃ 1-CN-cyclopropyl H O 0 A-1976 H H H H H CH₂CH₂SO₂CF₃ 1-CN-cyclopropyl H O 0 A-1977 H H H H H CH₂CH₂CH₂SO₂CF₃ 1-CN-cyclopropyl H O 0 A-1978 H H H H H CH₂C(═O)NHCH₂CHF₂ 1-CN-cyclopropyl H O 0 A-1979 H H H H H CH₂C(═O)NHCH₂CF₃ 1-CN-cyclopropyl H O 0 A-1980 H H H H H H CH₂OH H O 0 A-1981 H H H H H CH₃ CH₂OH H O 0 A-1982 H H H H H CH₂CH₃ CH₂OH H O 0 A-1983 H H H H H CH(CH₃)₃ CH₂OH H O 0 A-1984 H H H H H CH₂CH₂CH₃ CH₂OH H O 0 A-1985 H H H H H CH₂CH(CH₃)₂ CH₂OH H O 0 A-1986 H H H H H CH(CH₃)CH₂CH₃ CH₂OH H O 0 A-1987 H H H H H CH₂C(CH₃)₃ CH₂OH H O 0 A-1988 H H H H H CH₂(CH₂)₂CH₃ CH₂OH H O 0 A-1989 H H H H H CH₂(CH₂)₃CH₃ CH₂OH H O 0 A-1990 H H H H H CF₃ CH₂OH H O 0 A-1991 H H H H H CHF₂ CH₂OH H O 0 A-1992 H H H H H CH₂CF₃ CH₂OH H O 0 A-1993 H H H H H CH₂CHF₂ CH₂OH H O 0 A-1994 H H H H H CH₂CClF₂ CH₂OH H O 0 A-1995 H H H H H CH₂CBrF₂ CH₂OH H O 0 A-1996 H H H H H CF₂CF₃ CH₂OH H O 0 A-1997 H H H H H CH₂CHF₂ CH₂OH H O 0 A-1998 H H H H H CH₂CH₂CF₂ CH₂OH H O 0 A-1999 H H H H H CH₂CF₂CF₃ CH₂OH H O 0 A-2000 H H H H H CH₂CF₂CHF₂ CH₂OH H O 0 A-2001 H H H H H CF₂CHFCF₂ CH₂OH H O 0 A-2002 H H H H H CF₂CF₂CF₃ CH₂OH H O 0 A-2003 H H H H H CH₂CF₂CF₂CF₃ CH₂OH H O 0 A-2004 H H H H H CH₂CF₂CHFCF₃ CH₂OH H O 0 A-2005 H H H H H CH₂CH₂CH₂CF₃ CH₂OH H O 0 A-2006 H H H H H CH₂CH₂CF₂CF₃ CH₂OH H O 0 A-2007 H H H H H CF₂CF₂CF₂CF₃ CH₂OH H O 0 A-2008 H H H H H CH₂CH₂CH(CF₃)₂ CH₂OH H O 0

TABLE 34 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2009 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂OH H O 0 A-2010 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂OH H O 0 A-2011 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂OH H O 0 A-2012 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂OH H O 0 A-2013 H H H H H CH₂CH₂OCH₂CF₃ CH₂OH H O 0 A-2014 H H H H H CF₂CHFOCF₃ CH₂OH H O 0 A-2015 H H H H H CF₂CHFOCF₂CF₃ CH₂OH H O 0 A-2016 H H H H H CH₂CH₂CF═CF₂ CH₂OH H O 0 A-2017 H H H H H CH₂CH₂CH═CF₂ CH₂OH H O 0 A-2018 H H H H H CH₂C≡CCH₃ CH₂OH H O 0 A-2019 H H H H H CH₂C≡CCF₃ CH₂OH H O 0 A-2020 H H H H H CH₂C≡CI CH₂OH H O 0 A-2021 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂OH H O 0 A-2022 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂OH H O 0 A-2023 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂OH H O 0 A-2024 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂OH H O 0 A-2025 H H H H H CH₂SCH₃ CH₂OH H O 0 A-2026 H H H H H CH₂SCH₂CH₃ CH₂OH H O 0 A-2027 H H H H H CH₂CH₂SCH₃ CH₂OH H O 0 A-2028 H H H H H CH₂SOCH₃ CH₂OH H O 0 A-2029 H H H H H CH₂CH₂SOCH₃ CH₂OH H O 0 A-2030 H H H H H CH₂SO₂CH₃ CH₂OH H O 0 A-2031 H H H H H CH₂CH₂SO₂CH₃ CH₂OH H O 0 A-2032 H H H H H CH₂SCF₃ CH₂OH H O 0 A-2033 H H H H H CH₂SCHF₂ CH₂OH H O 0 A-2034 H H H H H CH₂SCH₂CF₃ CH₂OH H O 0 A-2035 H H H H H CH₂SCH₂CHF₂ CH₂OH H O 0 A-2036 H H H H H CH₂SCF₂CF₃ CH₂OH H O 0 A-2037 H H H H H CH₂CH₂SCF₃ CH₂OH H O 0 A-2038 H H H H H CH₂SOCF₃ CH₂OH H O 0 A-2039 H H H H H CH₂CH₂SOCF₃ CH₂OH H O 0 A-2040 H H H H H CH₂CH₂CH₂SOCF₂ CH₂OH H O 0 A-2041 H H H H H CH₂SO₂CF₃ CH₂OH H O 0 A-2042 H H H H H CH₂CH₂SO₂CF₃ CH₂OH H O 0 A-2043 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂OH H O 0 A-2044 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂OH H O 0 A-2045 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂OH H O 0 A-2046 H H H H H H NH₂ H O 0 A-2047 H H H H H CH₃ NH₂ H O 0 A-2048 H H H H H CH₂CH₃ NH₂ H O 0 A-2049 H H H H H CH(CH₃)₂ NH₂ H O 0 A-2050 H H H H H CH₂CH₂CH₃ NH₂ H O 0 A-2051 H H H H H CH₂CH(CH₃)₂ NH₂ H O 0 A-2052 H H H H H CH(CH₃)CH₂CH₃ NH₂ H O 0 A-2053 H H H H H CH₂C(CH₃)₃ NH₂ H O 0 A-2054 H H H H H CH₂(CH₂)₂CH₃ NH₂ H O 0 A-2055 H H H H H CH₂(CH₂)₃CH₃ NH₂ H O 0 A-2056 H H H H H CF₃ NH₂ H O 0 A-2057 H H H H H CHF₂ NH₂ H O 0 A-2058 H H H H H CH₂CF₃ NH₂ H O 0 A-2059 H H H H H CH₂CHF₂ NH₂ H O 0 A-2060 H H H H H CH₂CClF₂ NH₂ H O 0 A-2061 H H H H H CH₂CBrF₂ NH₂ H O 0 A-2062 H H H H H CF₂CF₃ NH₂ H O 0 A-2063 H H H H H CF₂CHF₂ NH₂ H O 0 A-2064 H H H H H CH₂CH₂CF₃ NH₂ H O 0 A-2065 H H H H H CH₂CF₂CF₃ NH₂ H O 0 A-2066 H H H H H CH₂CF₂CHF₂ NH₂ H O 0 A-2067 H H H H H CF₂CHFCF NH₂ H O 0 A-2068 H H H H H CF₂CF₂CF₃ NH₂ H O 0 A-2069 H H H H H CH₂CF₂CF₂CF₃ NH₂ H O 0

TABLE 35 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2070 H H H H H CH₂CF₂CHFCF₃ NH₂ H O 0 A-2071 H H H H H CH₂CH₂CH₂CF₃ NH₂ H O 0 A-2072 H H H H H CH₂CH₂CF₂CF₃ NH₂ H O 0 A-2073 H H H H H CF₂CF₂CF₂CF₃ NH₂ H O 0 A-2074 H H H H H CH₂CH₂CH(CF₃)₂ NH₂ H O 0 A-2075 H H H H H CF₂CF₂CF₂CF₂CF₃ NH₂ H O 0 A-2076 H H H H H CH₂CF₂CF₂CF₂CF₃ NH₂ H O 0 A-2077 H H H H H CH₂CH₂CH₂CH₂CF₃ NH₂ H O 0 A-2078 H H H H H CH₂CF₂CF₂CF₂CHF₂ NH₂ H O 0 A-2079 H H H H H CH₂CH₂OCH₂CF₃ NH₂ H O 0 A-2080 H H H H H CF₂CHFOCF₂ NH₂ H O 0 A-2081 H H H H H CF₂CHFOCH₂CF₃ NH₂ H O 0 A-2082 H H H H H CH₂CH₂CF═CF₂ NH₂ H O 0 A-2083 H H H H H CH₂CH₂CH═CF₂ NH₂ H O 0 A-2084 H H H H H CH₂C≡CCH₃ NH₂ H O 0 A-2085 H H H H H CH₂C≡CCF₃ NH₂ H O 0 A-2086 H H H H H CH₂C≡CI NH₂ H O 0 A-2087 H H H H H CH₂(2,2-difluorocyclopropyl) NH₂ H O 0 A-2088 H H H H H CH₂(2,2-dichlorocyclopropyl) NH₂ H O 0 A-2089 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) NH₂ H O 0 A-2090 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) NH₂ H O 0 A-2091 H H H H H CH₂SCH₃ NH₂ H O 0 A-2092 H H H H H CH₂SCH₂CH₃ NH₂ H O 0 A-2093 H H H H H CH₂CH₂SCH₃ NH₂ H O 0 A-2094 H H H H H CH₂SOCH₃ NH₂ H O 0 A-2095 H H H H H CH₂CH₂SOCH₃ NH₂ H O 0 A-2096 H H H H H CH₂SO₂CH₂ NH₂ H O 0 A-2097 H H H H H CH₂CH₂SO₂CH₃ NH₂ H O 0 A-2098 H H H H H CH₂SCF₃ NH₂ H O 0 A-2099 H H H H H CH₂SCHF₂ NH₂ H O 0 A-2100 H H H H H CH₂SCH₂CF₃ NH₂ H O 0 A-2101 H H H H H CH₂SCH₂CHF₂ NH₂ H O 0 A-2102 H H H H H CH₂SCF₂CF₃ NH₂ H O 0 A-2103 H H H H H CH₂CH₂SCF₂ NH₂ H O 0 A-2104 H H H H H CH₂SOCF₃ NH₂ H O 0 A-2105 H H H H H CH₂CH₂SOCF₃ NH₂ H O 0 A-2106 H H H H H CH₂CH₂CH₂SOCF₃ NH₂ H O 0 A-2107 H H H H H CH₂SO₂CF₃ NH₂ H O 0 A-2108 H H H H H CH₂CH₂SO₂CF₃ NH₂ H O 0 A-2109 H H H H H CH₂CH₂CH₂SO₂CF₃ NH₂ H O 0 A-2110 H H H H H CH₂C(═O)NHCH₂CHF₂ NH₂ H O 0 A-2111 H H H H H CH₂C(═O)NHCH₂CF₃ NH₂ H O 0 A-2112 H H H H H H C(═O)CH₃ H O 0 A-2113 H H H H H CH₃ C(═O)CH₃ H O 0 A-2114 H H H H H CH₂CH₃ C(═O)CH₃ H O 0 A-2115 H H H H H CH(CH₃)₂ C(═O)CH₃ H O 0 A-2116 H H H H H CH₂CH₂CH₃ C(═O)CH₃ H O 0 A-2117 H H H H H CH₂CH(CH₃)₂ C(═O)CH₃ H O 0 A-2118 H H H H H CH₂C(CH₃)₃ C(═O)CH₃ H O 0 A-2119 H H H H H CH(CH₃)CH₂CH₃ C(═O)CH₃ H O 0 A-2120 H H H H H CH₂(CH₂)₂CH₃ C(═O)CH₃ H O 0 A-2121 H H H H H CH₂(CH₂)₃CH₃ C(═O)CH₃ H O 0 A-2122 H H H H H CH₂(CH₂)₄CH₃ C(═O)CH₃ H O 0 A-2123 H H H H H CH₂(CH₂)₆CH₃ C(═O)CH₃ H O 0 A-2124 H H H H H CH₂OCH₃ C(═O)CH₃ H O 0 A-2125 H H H H H CH₂OCH₂CH₃ C(═O)CH₃ H O 0 A-2126 H H H H H CH₂CH₂OCH₃ C(═O)CH₃ H O 0 A-2127 H H H H H CH₂CH₂OCH₂CH₃ C(═O)CH₃ H O 0 A-2128 H H H H H CF₃ C(═O)CH₃ H O 0 A-2129 H H H H H CHF₂ C(═O)CH₃ H O 0 A-2130 H H H H H CH₂CF₃ C(═O)CH₃ H O 0

TABLE 36 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2131 H H H H H CH₂CHF₂ C(═O)CH₃ H O 0 A-2132 H H H H H CH₂CClF₂ C(═O)CH₃ H O 0 A-2133 H H H H H CH₂CBrF₂ C(═O)CH₃ H O 0 A-2134 H H H H H CF₂CF₃ C(═O)CH₃ H O 0 A-2135 H H H H H CF₂CHF₂ C(═O)CH₃ H O 0 A-2136 H H H H H CH₂CH₂CF₃ C(═O)CH₃ H O 0 A-2137 H H H H H CH₂CF₂CF₃ C(═O)CH₃ H O 0 A-2138 H H H H H CH₂CF₂CHF₂ C(═O)CH₃ H O 0 A-2139 H H H H H CF₂CHFCF₃ C(═O)CH₃ H O 0 A-2140 H H H H H CF₂CF₂CF₃ C(═O)CH₃ H O 0 A-2141 H H H H H CH₂CF₂CF₂CF₃ C(═O)CH₃ H O 0 A-2142 H H H H H CH₂CF₂CHFCF₃ C(═O)CH₃ H O 0 A-2143 H H H H H CH₂CH₂CH₂CF₃ C(═O)CH₃ H O 0 A-2144 H H H H H CH₂CH₂CF₂CF₃ C(═O)CH₃ H O 0 A-2145 H H H H H CF₂CF₂CF₂CF₃ C(═O)CH₃ H O 0 A-2146 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)CH₃ H O 0 A-2147 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)CH₃ H O 0 A-2148 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)CH₃ H O 0 A-2149 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)CH₃ H O 0 A-2150 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)CH₃ H O 0 A-2151 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ C(═O)CH₃ H O 0 A-2152 H H H H H CF₂CHFOCH₃ C(═O)CH₃ H O 0 A-2153 H H H H H CF₂CHFOCH₂CH₃ C(═O)CH₃ H O 0 A-2154 H H H H H CH₂CH₂OCH₂CF₃ C(═O)CH₃ H O 0 A-2155 H H H H H CF₂CHFOCF₃ C(═O)CH₃ H O 0 A-2156 H H H H H CF₂CHFOCF₂CF₃ C(═O)CH₃ H O 0 A-2157 H H H H H CF₂CHFOCF₂CF₂CF₃ C(═O)CH₃ H O 0 A-2158 H H H H H CH₂CH═CH₂ C(═O)CH₃ H O 0 A-2159 H H H H H CH₂CH═CHCl C(═O)CH₃ H O 0 A-2160 H H H H H CH₂CH═CCl₂ C(═O)CH₃ H O 0 A-2161 H H H H H CH₂CH₂CF═CF₂ C(═O)CH₃ H O 0 A-2162 H H H H H CH₂CH₂CH═CF₂ C(═O)CH₃ H O 0 A-2163 H H H H H CH₂C≡CH C(═O)CH₃ H O 0 A-2164 H H H H H CH₂C≡CCH₃ C(═O)CH₃ H O 0 A-2165 H H H H H CH₂C≡CI C(═O)CH₃ H O 0 A-2166 H H H H H CH₂C≡CCF₃ C(═O)CH₃ H O 0 A-2167 H H H H H cyclobutyl C(═O)CH₃ H O 0 A-2168 H H H H H cyclopentyl C(═O)CH₃ H O 0 A-2169 H H H H H cyclohexyl C(═O)CH₃ H O 0 A-2170 H H H H H 4,4-difluorocyclohexyl C(═O)CH₃ H O 0 A-2171 H H H H H CH₂(cyclopropyl) C(═O)CH₃ H O 0 A-2172 H H H H H CH₂(cyclobutyl) C(═O)CH₃ H O 0 A-2173 H H H H H CH₂(cyclopentyl) C(═O)CH₃ H O 0 A-2174 H H H H H CH₂CH₂(cyclopropyl) C(═O)CH₃ H O 0 A-2175 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)CH₃ H O 0 A-2176 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)CH₃ H O 0 A-2177 H H H H H CH₂(4,4-difluorocyclohexyl) C(═O)CH₃ H O 0 A-2178 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)CH₃ H O 0 A-2179 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)CH₃ H O 0 A-2180 H H H H H CH₂SCH₃ C(═O)CH₃ H O 0 A-2181 H H H H H CH₂SCH₂CH₃ C(═O)CH₃ H O 0 A-2182 H H H H H CH₂CH₂SCH₃ C(═O)CH₃ H O 0 A-2183 H H H H H CH₂CH₂SCH₂CH₃ C(═O)CH₃ H O 0 A-2184 H H H H H CH₂CH₂CH₂SCH₃ C(═O)CH₃ H O 0 A-2185 H H H H H CH₂CH₂CH₂SCH₂CH₃ C(═O)CH₃ H O 0 A-2186 H H H H H CH(CH₃)SCH₃ C(═O)CH₃ H O 0 A-2187 H H H H H CH(CH₃)SCH₂CH₃ C(═O)CH₃ H O 0 A-2188 H H H H H CH₂CH(CH₃)SCH₃ C(═O)CH₃ H O 0 A-2189 H H H H H CH₂CH(CH₃)SCH₂CH₃ C(═O)CH₃ H O 0 A-2190 H H H H H CH(CH₃)CH₂CH₂SCH₃ C(═O)CH₃ H O 0 A-2191 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ C(═O)CH₃ H O 0

TABLE 37 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2192 H H H H H CH₂CH(CH₃)CH₂SCH₃ C(═O)CH₃ H O 0 A-2193 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ C(═O)CH₃ H O 0 A-2194 H H H H H CH₂CH₂CH(CH₃)SCH₃ C(═O)CH₃ H O 0 A-2195 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ C(═O)CH₃ H O 0 A-2196 H H H H H CH₂SOCH₃ C(═O)CH₃ H O 0 A-2197 H H H H H CH₂CH₂SOCH₃ C(═O)CH₃ H O 0 A-2198 H H H H H CH₂CH₂CH₂SOCH₃ C(═O)CH₃ H O 0 A-2199 H H H H Id CH(CH₃)SOCH₃ C(═O)CH₃ H O 0 A-2200 H H H H H CH₂CH(CH₃)SOCH₃ C(═O)CH₃ H O 0 A-2201 H H H H H CH(CH₃)CH₂CH₂SOCH₃ C(═O)CH₃ H O 0 A-2202 H H H H H CH₂CH(CH₃)CH₂SOCH₃ C(═O)CH₃ H O 0 A-2203 H H H H H CH₂CH₂CH(CH₃)SOCH₃ C(═O)CH₃ H O 0 A-2204 H H H H H CH₂SO₂CH₃ C(═O)CH₃ H O 0 A-2205 H H H H H CH₂CH₂SO₂CH₃ C(═O)CH₃ H O 0 A-2206 H H H H H CH₂CH₂CH₂SO₂CH₃ C(═O)CH₃ H O 0 A-2207 H H H H H CH(CH₃)SO₂CH₃ C(═O)CH₃ H O 0 A-2208 H H H H H CH₂CH(CH₃)SO₂CH₃ C(═O)CH₃ H O 0 A-2209 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ C(═O)CH₃ H O 0 A-2210 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ C(═O)CH₃ H O 0 A-2211 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ C(═O)CH₃ H O 0 A-2212 H H H H H CH₂SCF₃ C(═O)CH₃ H O 0 A-2213 H H H H H CH₂SCHF₂ C(═O)CH₃ H O 0 A-2214 H H H H H CH₂SCH₂CF₃ C(═O)CH₃ H O 0 A-2215 H H H H H CH₂SCH₂CHF₂ C(═O)CH₃ H O 0 A-2216 H H H H H CH₂SCF₂CF₃ C(═O)CH₃ H O 0 A-2217 H H H H H CH₂CH₂SCF₃ C(═O)CH₃ H O 0 A-2218 H H H H H CH₂CH₂SCH₂CF₃ C(═O)CH₃ H O 0 A-2219 H H H H H CH₂CH₂CH₂SCF₃ C(═O)CH₃ H O 0 A-2220 H H H H H CH₂CH₂CH₂SCH₂CF₃ C(═O)CH₃ H O 0 A-2221 H H H H H CH(CH₃)SCF₃ C(═O)CH₃ H O 0 A-2222 H H H H H CH(CH₃)SCH₂CF₃ C(═O)CH₃ H O 0 A-2223 H H H H H CH₂CH(CH₃)SCF₃ C(═O)CH₃ H O 0 A-2224 H H H H H CH₂CH(CH₃)SCH₂CF₃ C(═O)CH₃ H O 0 A-2225 H H H H H CH(CH₃)CH₂CH₂SCF₃ C(═O)CH₃ H O 0 A-2226 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ C(═O)CH₃ H O 0 A-2227 H H H H H CH₂CH(CH₃)CH₂SCF₃ C(═O)CH₃ H O 0 A-2228 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ C(═O)CH₃ H O 0 A-2229 H H H H H CH₂CH₂CH(CH₃)SCF₃ C(═O)CH₃ H O 0 A-2230 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ C(═O)CH₃ H O 0 A-2231 H H H H H CH₂SOCF₃ C(═O)CH₃ H O 0 A-2232 H H H H H CH₂CH₂SOCF₃ C(═O)CH₃ H O 0 A-2233 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)CH₃ H O 0 A-2234 H H H H H CH(CH₃)SOCF₃ C(═O)CH₃ H O 0 A-2235 H H H H H CH₂CH(CH₃)SOCF₃ C(═O)CH₃ H O 0 A-2236 H H H H H CH(CH₃)CH₂CH₂SOCF₃ C(═O)CH₃ H O 0 A-2237 H H H H H CH₂CH(CH₃)CH₂SOCF₃ C(═O)CH₃ H O 0 A-2238 H H H H H CH₂CH₂CH(CH₃)SOCF₃ C(═O)CH₃ H O 0 A-2239 H H H H H CH₂SO₂CF₃ C(═O)CH₃ H O 0 A-2240 H H H H H CH₂CH₂SO₂CF₃ C(═O)CH₃ H O 0 A-2241 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)CH₃ H O 0 A-2242 H H H H H CH(CH₃)SO₂CF₃ C(═O)CH₃ H O 0 A-2243 H H H H H CH₂CH(CH₃)SO₂CF₃ C(═O)CH₃ H O 0 A-2244 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ C(═O)CH₃ H O 0 A-2245 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ C(═O)CH₃ H O 0 A-2246 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ C(═O)CH₃ H O 0 A-2247 H H H H H CH₂C(═O)CH₃ C(═O)CH₃ H O 0 A-2248 H H H H H CH₂C(═O)CH₂CH₃ C(═O)CH₃ H O 0 A-2249 H H H H H CH₂C(═O)C(CH₃)₃ C(═O)CH₃ H O 0 A-2250 H H H H H CH₂CH₂C(═O)CH₃ C(═O)CH₃ H O 0 A-2251 H H H H H CH₂CH₂C(═O)C(CH₃)₃ C(═O)CH₃ H O 0 A-2252 H H H H H CH₂C(═O)CF₃ C(═O)CH₃ H O 0

TABLE 38 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2253 H H H H H CH₂CH₂C(═O)CF₃ C(═O)CH₃ H O 0 A-2254 H H H H H CH₂C(═O)OCH₃ C(═O)CH₃ H O 0 A-2255 H H H H H CH₂C(═O)OCH₂CH₃ C(═O)CH₃ H O 0 A-2256 H H H H H CH₂C(═O)OC(CH₃)₃ C(═O)CH₃ H O 0 A-2257 H H H H H CH₂CH₂C(═O)OCH₃ C(═O)CH₃ H O 0 A-2258 H H H H H CH₂CH₂C(═O)OCH₂CH₃ C(═O)CH₃ H O 0 A-2259 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ C(═O)CH₃ H O 0 A-2260 H H H H H CH₂C(═O)NH₂ C(═O)CH₃ H O 0 A-2261 H H H H H CH₂CH₂C(═O)NH₂ C(═O)CH₃ H O 0 A-2262 H H H H H CH₂C(═O)NHCH₃ C(═O)CH₃ H O 0 A-2263 H H H H H CH₂C(═O)NHCH(CH₃)₂ C(═O)CH₃ H O 0 A-2264 H H H H H CH₂CH₂C(═O)NHCH₃ C(═O)CH₃ H O 0 A-2265 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ C(═O)CH₃ H O 0 A-2266 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)CH₃ H O 0 A-2267 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)CH₃ H O 0 A-2268 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ C(═O)CH₃ H O 0 A-2269 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ C(═O)CH₃ H O 0 A-2270 H H H H H CH₂C(═O)N(CH₃)₂ C(═O)CH₃ H O 0 A-2271 H H H H H CH₂C(═O)N(CH₂CH₃)₂ C(═O)CH₃ H O 0 A-2272 H H H H H CH₂CH₂C(═O)N(CH₃)₂ C(═O)CH₃ H O 0 A-2273 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ C(═O)CH₃ H O 0 A-2274 H H H H H CH₂CH₂OH C(═O)CH₃ H O 0 A-2275 H H H H H CH₂CH(OH)CH₃ C(═O)CH₃ H O 0 A-2276 H H H H H CH₂CH₂CH₂OH C(═O)CH₃ H O 0 A-2277 H H H H H CH₂CH(OH)CH₂CH₃ C(═O)CH₃ H O 0 A-2278 H H H H H CH₂CH(OH)C(CH₃)₃ C(═O)CH₃ H O 0 A-2279 H H H H H CH₂CH₂CH(OH)CH₃ C(═O)CH₃ H O 0 A-2280 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ C(═O)CH₃ H O 0 A-2281 H H H H H CH₂C(═NOH)CH₃ C(═O)CH₃ H O 0 A-2282 H H H H H CH₂C(═NOH)CH₂CH₃ C(═O)CH₃ H O 0 A-2283 H H H H H CH₂C(═NOH)C(CH₃)₃ C(═O)CH₃ H O 0 A-2284 H H H H H CH₂C(═NOCH₃)CH₃ C(═O)CH₃ H O 0 A-2285 H H H H H CH₂C(═NOCH₃)CH₂CH₃ C(═O)CH₃ H O 0 A-2286 H H H H H CH₂C(═NOCH₂CH₃)CH₃ C(═O)CH₃ H O 0 A-2287 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ C(═O)CH₃ H O 0 A-2288 H H H H H CH₂C(═NOCH₂CF₃)CH₃ C(═O)CH₃ H O 0 A-2289 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ C(═O)CH₃ H O 0 A-2290 H H H H H CH₂Ph C(═O)CH₃ H O 0 A-2291 H H H H H CH₂(2-F)Ph C(═O)CH₃ H O 0 A-2292 H H H H H CH₂(3-F)Ph C(═O)CH₃ H O 0 A-2293 H H H H H CH₂(4-F)Ph C(═O)CH₃ H O 0 A-2294 H H H H H CH₂(2-Cl)Ph C(═O)CH₃ H O 0 A-2295 H H H H H CH₂(3-Cl)Ph C(═O)CH₃ H O 0 A-2296 H H H H H CH₂(4-Cl)Ph C(═O)CH₃ H O 0 A-2297 H H H H H CH₂(2-CF₃)Ph C(═O)CH₃ H O 0 A-2298 H H H H H CH₂(3-CF₃)Ph C(═O)CH₃ H O 0 A-2299 H H H H H CH₂(4-CF₃)Ph C(═O)CH₃ H O 0 A-2300 H H H H H CH₂(naphthalen-1-yl) C(═O)CH₃ H O 0 A-2301 H H H H H CH₂(naphtnalen-2-yl) C(═O)CH₃ H O 0 A-2302 H H H H H CH₂CH₂Ph C(═O)CH₃ H O 0 A-2303 H H H H H H C(═O)CH₂CH₃ H O 0 A-2304 H H H H H CH₃ C(═O)CH₂CH₃ H O 0 A-2305 H H H H H CH₂CH₃ C(═O)CH₂CH₃ H O 0 A-2306 H H H H H CH(CH₃)₂ C(═O)CH₂CH₃ H O 0 A-2307 H H H H H CH₂CH₂CH₃ C(═O)CH₂CH₃ H O 0 A-2308 H H H H H CH₂CH(CH₃)₂ C(═O)CH₂CH₃ H O 0 A-2309 H H H H H CH(CH₃)CH₂CH₃ C(═O)CH₂CH₃ H O 0 A-2310 H H H H H CH₂C(CH₃)₃ C(═O)CH₂CH₃ H O 0 A-2311 H H H H H CH₂(CH₂)₂CH₃ C(═O)CH₂CH₃ H O 0 A-2312 H H H H H CH₂(CH₂)₃CH₃ C(═O)CH₂CH₃ H O 0 A-2313 H H H H H CF₃ C(═O)CH₂CH₃ H O 0

TABLE 39 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2314 H H H H H CHF₂ C(═O)CH₂CH₃ H O 0 A-2315 H H H H H CH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2316 H H H H H CH₂CHF₂ C(═O)CH₂CH₃ H O 0 A-2317 H H H H H CH₂CClF₂ C(═O)CH₂CH₃ H O 0 A-2318 H H H H H CH₂CBrF₂ C(═O)CH₂CH₃ H O 0 A-2319 H H H H H CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2320 H H H H H CF₂CHF₂ C(═O)CH₂CH₃ H O 0 A-2321 H H H H H CH₂CH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2322 H H H H H CH₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2323 H H H H H CH₂CF₂CHF₂ C(═O)CH₂CH₃ H O 0 A-2324 H H H H H CF₂CHFCF₃ C(═O)CH₂CH₃ H O 0 A-2325 H H H H H CF₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2326 H H H H H CH₂CF₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2327 H H H H H CH₂CF₂CHFCF₃ C(═O)CH₂CH₃ H O 0 A-2328 H H H H H CH₂CH₂CH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2329 H H H H H CH₂CH₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2330 H H H H H CF₂CF₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2331 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)CH₂CH₃ H O 0 A-2332 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2333 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2334 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2335 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)CH₂CH₃ H O 0 A-2336 H H H H H CH₂CH₂OCH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2337 H H H H H CF₂CHFOCF₃ C(═O)CH₂CH₃ H O 0 A-2338 H H H H H CF₂CHFOCF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2339 H H H H H CH₂CH₂CF═CF₂ C(═O)CH₂CH₃ H O 0 A-2340 H H H H H CH₂CH₂CH═CF₂ C(═O)CH₂CH₃ H O 0 A-2341 H H H H H CH₂C≡CCH₃ C(═O)CH₂CH₃ H O 0 A-2342 H H H H H CH₂C≡CCF₃ C(═O)CH₂CH₃ H O 0 A-2343 H H H H H CH₂C≡CI C(═O)CH₂CH₃ H O 0 A-2344 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)CH₂CH₃ H O 0 A-2345 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)CH₂CH₃ H O 0 A-2346 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)CH₂CH₃ H O 0 A-2347 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)CH₂CH₃ H O 0 A-2348 H H H H H CH₂SCH₃ C(═O)CH₂CH₃ H O 0 A-2349 H H H H H CH₂SCH₂CH₃ C(═O)CH₂CH₃ H O 0 A-2350 H H H H H CH₂CH₂SCH₃ C(═O)CH₂CH₃ H O 0 A-2351 H H H H H CH₂SOCH₃ C(═O)CH₂CH₃ H O 0 A-2352 H H H H H CH₂CH₂SOCH₃ C(═O)CH₂CH₃ H O 0 A-2353 H H H H H CH₂SO₂CH₃ C(═O)CH₂CH₃ H O 0 A-2354 H H H H H CH₂CH₂SO₂CH₃ C(═O)CH₂CH₃ H O 0 A-2355 H H H H H CH₂SCF₃ C(═O)CH₂CH₃ H O 0 A-2356 H H H H H CH₂SCHF₂ C(═O)CH₂CH₃ H O 0 A-2357 H H H H H CH₂SCH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2358 H H H H H CH₂SCH₂CHF₂ C(═O)CH₂CH₃ H O 0 A-2359 H H H H H CH₂SCF₂CF₃ C(═O)CH₂CH₃ H O 0 A-2360 H H H H H CH₂CH₂SCF₃ C(═O)CH₂CH₃ H O 0 A-2361 H H H H H CH₂SOCF₃ C(═O)CH₂CH₃ H O 0 A-2362 H H H H H CH₂CH₂SOCF₃ C(═O)CH₂CH₃ H O 0 A-2363 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)CH₂CH₃ H O 0 A-2364 H H H H H CH₂SO₂CF₃ C(═O)CH₂CH₃ H O 0 A-2365 H H H H H CH₂CH₂SO₂CF₃ C(═O)CH₂CH₃ H O 0 A-2366 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)CH₂CH₃ H O 0 A-2367 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)CH₂CH₃ H O 0 A-2368 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)CH₂CH₃ H O 0 A-2369 H H H H H H C(═O)CH(CH₃)₂ H O 0 A-2370 H H H H H CH₃ C(═O)CH(CH₃)₂ H O 0 A-2371 H H H H H CH₂CH₃ C(═O)CH(CH₃)₂ H O 0 A-2372 H H H H H CH(CH₃)₂ C(═O)CH(CH₃)₂ H O 0 A-2373 H H H H H CH₂CH₂CH₃ C(═O)CH(CH₃)₂ H O 0 A-2374 H H H H H CH₂CH(CH₃)₂ C(═O)CH(CH3)₂ H O 0

TABLE 40 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2375 H H H H H CH(CH₃)CH₂CH₃ C(═O)CH(CH₃)₂ H O 0 A-2376 H H H H H CH₂C(CH₃)₃ C(═O)CH(CH₃)₂ H O 0 A-2377 H H H H H CH₂(CH₂)₂CH₃ C(═O)CH(CH₃)₂ H O 0 A-2378 H H H H H CH₂(CH₂)₃CH₃ C(═O)CH(CH₃)₂ H O 0 A-2379 H H H H H CF₃ C(═O)CH(CH₃)₂ H O 0 A-2380 H H H H H CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2381 H H H H H CH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2382 H H H H H CH₂CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2383 H H H H H CH₂CClF₂ C(═O)CH(CH₃)₂ H O 0 A-2384 H H H H H CH₂CBrF₂ C(═O)CH(CH₃)₂ H O 0 A-2385 H H H H H CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2386 H H H H H CF₂CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2387 H H H H H CH₂CH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2388 H H H H H CH₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2389 H H H H H CH₂CF₂CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2390 H H H H H CF₂CHFCF₃ C(═O)CH(CH₃)₂ H O 0 A-2391 H H H H H CF₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2392 H H H H H CH₂CF₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2393 H H H H H CH₂CF₂CHFCF₃ C(═O)CH(CH₃)₂ H O 0 A-2394 H H H H H CH₂CH₃CH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2395 H H H H H CH₂CH₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2396 H H H H H CF₂CF₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2397 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)CH(CH₃)₂ H O 0 A-2398 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2399 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2400 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2401 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2402 H H H H H CH₂CH₂OCH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2403 H H H H H CF₂CHFOCF₃ C(═O)CH(CH₃)₂ H O 0 A-2404 H H H H H CF₂CHFOCF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2405 H H H H H CH₂CH₂CF═CF₂ C(═O)CH(CH₃)₂ H O 0 A-2406 H H H H H CH₂CH₂CH═CF₂ C(═O)CH(CH₃)₂ H O 0 A-2407 H H H H H CH₂C≡CCH₃ C(═O)CH(CH₃)₂ H O 0 A-2408 H H H H H CH₂C≡CCF₃ C(═O)CH(CH₃)₂ H O 0 A-2409 H H H H H CH₂C≡CI C(═O)CH(CH₃)₂ H O 0 A-2410 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)CH(CH₃)₂ H O 0 A-2411 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)CH(CH₃)₂ H O 0 A-2412 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)CH(CH₃)₂ H O 0 A-2413 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)CH(CH₃)₂ H O 0 A-2414 H H H H H CH₂SCH₃ C(═O)CH(CH₃)₂ H O 0 A-2415 H H H H H CH₂SCH₂CH₃ C(═O)CH(CH₃)₂ H O 0 A-2416 H H H H H CH₂CH₂SCH₃ C(═O)CH(CH₃)₂ H O 0 A-2417 H H H H H CH₂SOCH₃ C(═O)CH(CH₃)₂ H O 0 A-2418 H H H H H CH₂CH₂SOCH₃ C(═O)CH(CH₃)₂ H O 0 A-2419 H H H H H CH₂SO₂CH₃ C(═O)CH(CH₃)₂ H O 0 A-2420 H H H H H CH₂CH₂SO₃CH₃ C(═O)CH(CH₃)₂ H O 0 A-2421 H H H H H CH₂SCF₃ C(═O)CH(CH₃)₂ H O 0 A-2422 H H H H H CH₂SCHF₂ C(═O)CH(CH₃)₂ H O 0 A-2423 H H H H H CH₂SCH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2424 H H H H H CH₂SCH₂CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2425 H H H H H CH₂SCF₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2426 H H H H H CH₂CH₂SCF₃ C(═O)CH(CH₃)₂ H O 0 A-2427 H H H H H CH₂SOCF₃ C(═O)CH(CH₃)₂ H O 0 A-2428 H H H H H CH₂CH₂SOCF₃ C(═O)CH(CH₃)₂ H O 0 A-2429 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)CH(CH₃)₂ H O 0 A-2430 H H H H H CH₂SO₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2431 H H H H H CH₂CH₂SO₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2432 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2433 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)CH(CH₃)₂ H O 0 A-2434 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)CH(CH₃)₂ H O 0 A-2435 H H H H H H C(═O)CH₂OCH₃ H O 0

TABLE 41 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2436 H H H H H CH₃ C(═O)CH₂OCH₃ H O 0 A-2437 H H H H H CH₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2438 H H H H H CH(CH₃)₂ C(═O)CH₂OCH₃ H O 0 A-2439 H H H H H CH₂CH₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2440 H H H H H CH₂CH(CH₃)₂ C(═O)CH₂OCH₃ H O 0 A-2441 H H H H H CH(CH₃)CH₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2442 H H H H H CH₂C(CH₃)₃ C(═O)CH₂OCH₃ H O 0 A-2443 H H H H H CH₂(CH₂)₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2444 H H H H H CH₂(CH₂)₃CH₃ C(═O)CH₂OCH₃ H O 0 A-2445 H H H H H CF₃ C(═O)CH₂OCH₃ H O 0 A-2446 H H H H H CHF₂ C(═O)CH₂OCH₃ H O 0 A-2447 H H H H H CH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2448 H H H H H CH₂CHF₂ C(═O)CH₂OCH₃ H O 0 A-2449 H H H H H CH₂CClF₂ C(═O)CH₂OCH₃ H O 0 A-2450 H H H H H CH₂CBrF₂ C(═O)CH₂OCH₃ H O 0 A-2451 H H H H H CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2452 H H H H H CF₂CHF₂ C(═O)CH₂OCH₃ H O 0 A-2453 H H H H H CH₂CH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2454 H H H H H CH₂CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2455 H H H H H CH₂CF₂CHF₂ C(═O)CH₂OCH₃ H O 0 A-2456 H H H H H CF₂CHFCF₃ C(═O)CH₂OCH₃ H O 0 A-2457 H H H H H CF₂CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2458 H H H H H CH₂CF₂CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2459 H H H H H CH₂CF₂CHFCF₃ C(═O)CH₂OCH₃ H O 0 A-2460 H H H H H CH₂CH₂CH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2461 H H H H H CH₂CH₂CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2462 H H H H H CF₂CF₂CE₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2463 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)CH₂OCH₃ H O 0 A-2464 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2465 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2466 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2467 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)CH₂OCH₃ H O 0 A-2468 H H H H H CH₂CH₂OCH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2469 H H H H H CF₂CHFOCF₃ C(═O)CH₂OCH₃ H O 0 A-2470 H H H H H CF₂CHFOCF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2471 H H H H H CH₂CH₂CF═CF₂ C(═O)CH₂OCH₃ H O 0 A-2472 H H H H H CH₂CH₂CH═CF₂ C(═O)CH₂OCH₃ H O 0 A-2473 H H H H H CH₂C≡CCH₃ C(═O)CH₂OCH₃ H O 0 A-2474 H H H H H CH₂C≡CCF₃ C(═O)CH₂OCH₃ H O 0 A-2475 H H H H H CH₂C≡CI C(═O)CH₂OCH₃ H O 0 A-2476 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)CH₂OCH₃ H O 0 A-2477 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)CH₂OCH₃ H O 0 A-2478 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)CH₂OCH₃ H O 0 A-2479 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)CH₂OCH₃ H O 0 A-2480 H H H H H CH₂SCH₃ C(═O)CH₂OCH₃ H O 0 A-2481 H H H H H CH₂SCH₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2482 H H H H H CH₂CH₂SCH₃ C(═O)CH₂OCH₃ H O 0 A-2483 H H H H H CH₂SOCH₃ C(═O)CH₂OCH₃ H O 0 A-2484 H H H H H CF₂CH₂SOCH₃ C(═O)CH₂OCH₃ H O 0 A-2485 H H H H H CH₂SO₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2486 H H H H H CH₂CH₂SO₂CH₃ C(═O)CH₂OCH₃ H O 0 A-2487 H H H H H CH₂SCF₃ C(═O)CH₂OCH₃ H O 0 A-2488 H H H H H CH₂SCHF₂ C(═O)CH₂OCH₃ H O 0 A-2489 H H H H H CH₂SCH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2490 H H H H H CH₂SCH₂CHF₂ C(═O)CH₂OCH₃ H O 0 A-2491 H H H H H CH₂SCF₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2492 H H H H H CH₂CH₂SCF₃ C(═O)CH₂OCH₃ H O 0 A-2493 H H H H H CH₂SOCF₃ C(═O)CH₂OCH₃ H O 0 A-2494 H H H H H CH₂CH₂SOCF₃ C(═O)CH₂OCH₃ H O 0 A-2495 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)CH₂OCH₃ H O 0 A-2496 H H H H H CH₂SO₂CF₃ C(═O)CH₂OCH₃ H O 0

TABLE 42 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2497 H H H H H CH₂CH₂SO₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2498 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2499 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)CH₂OCH₃ H O 0 A-2500 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)CH₂OCH₃ H O 0 A-2501 H H H H H H C(═O)cyclopropyl H O 0 A-2502 H H H H H CH₃ C(═O)cyclopropyl H O 0 A-2503 H H H H H CH₂CH₃ C(═O)cyclopropyl H O 0 A-2504 H H H H H CH(CH₃)₂ C(═O)cyclopropyl H O 0 A-2505 H H H H H CH₂CH₂CH₃ C(═O)cyclopropyl H O 0 A-2506 H H H H H CH₂CH(CH₃)₂ C(═O)cyclopropyl H O 0 A-2507 H H H H H CH(CH₃)CH₂CH₃ C(═O)cyclopropyl H O 0 A-2508 H H H H H CH₂C(CH₃)₃ C(═O)cyclopropyl H O 0 A-2509 H H H H H CH₂(CH₂)₂CH₃ C(═O)cyclopropyl H O 0 A-2510 H H H H H CH₂(CH₂)₃CH₃ C(═O)cyclopropyl H O 0 A-2511 H H H H H CF₃ C(═O)cyclopropyl H O 0 A-2512 H H H H H CHF₂ C(═O)cyclopropyl H O 0 A-2513 H H H H H CH₂CF₃ C(═O)cyclopropyl H O 0 A-2514 H H H H H CH₂CHF₂ C(═O)cyclopropyl H O 0 A-2515 H H H H H CH₂CClF₂ C(═O)cyclopropyl H O 0 A-2516 H H H H H CH₂CBrF₂ C(═O)cyclopropyl H O 0 A-2517 H H H H H CF₂CF₃ C(═O)cyclopropyl H O 0 A-2518 H H H H H CF₂CHF₂ C(═O)cyclopropyl H O 0 A-2519 H H H H H CH₂CH₂CF₃ C(═O)cyclopropyl H O 0 A-2520 H H H H H CH₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2521 H H H H H CH₂CF₂CHF₂ C(═O)cyclopropyl H O 0 A-2522 H H H H H CF₂CHFCF₃ C(═O)cyclopropyl H O 0 A-2523 H H H H H CF₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2524 H H H H H CH₂CF₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2525 H H H H H CH₂CF₂CHFCF₃ C(═O)cyclopropyl H O 0 A-2526 H H H H H CH₂CH₂CH₂CF₃ C(═O)cyclopropyl H O 0 A-2527 H H H H H CH₂CH₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2528 H H H H H CF₂CF₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2529 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)cyclopropyl H O 0 A-2530 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2531 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)cyclopropyl H O 0 A-2532 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)cyclopropyl H O 0 A-2533 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)cyclopropyl H O 0 A-2534 H H H H H CH₂CH₂OCH₂CF₃ C(═O)cyclopropyl H O 0 A-2535 H H H H H CF₂CHFOCF₃ C(═O)cyclopropyl H O 0 A-2536 H H H H H CF₂CHFOCF₂CF₃ C(═O)cyclopropyl H O 0 A-2537 H H H H H CH₂CH₂CF═CF₂ C(═O)cyclopropyl H O 0 A-2538 H H H H H CH₂CH₂CH═CF₂ C(═O)cyclopropyl H O 0 A-2539 H H H H H CH₂C≡CCH₃ C(═O)cyclopropyl H O 0 A-2540 H H H H H CH₂C≡CCF₃ C(═O)cyclopropyl H O 0 A-2541 H H H H H CH₂C≡CI C(═O)cyclopropyl H O 0 A-2542 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)cyclopropyl H O 0 A-2543 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)cyclopropyl H O 0 A-2544 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)cyclopropyl H O 0 A-2545 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)cyclopropyl H O 0 A-2546 H H H H H CH₂SCH₃ C(═O)cyclopropyl H O 0 A-2547 H H H H H CH₂SCH₂CH₃ C(═O)cyclopropyl H O 0 A-2548 H H H H H CH₂CH₂SCH₃ C(═O)cyclopropyl H O 0 A-2549 H H H H H CH₂SOCH₃ C(═O)cyclopropyl H O 0 A-2550 H H H H H CH₂CH₂SOCH₃ C(═O)cyclopropyl H O 0 A-2551 H H H H H CH₂SO₂CH₃ C(═O)cyclopropyl H O 0 A-2552 H H H H H CH₂CH₂SO₂CH₃ C(═O)cyclopropyl H O 0 A-2553 H H H H H CH₂SCF₃ C(═O)cyclopropyl H O 0 A-2554 H H H H H CH₂SCHF₂ C(═O)cyclopropyl H O 0 A-2555 H H H H H CH₂SCH₂CF₃ C(═O)cyclopropyl H O 0 A-2556 H H H H H CH₂SCH₂CHF₂ C(═O)cyclopropyl H O 0 A-2557 H H H H H CH₂SCF₂CF₃ C(═O)cyclopropyl H O 0

TABLE 43 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2558 H H H H H CH₂CH₂SCF₃ C(═O)cyclopropyl H O 0 A-2559 H H H H H CH₂SOCF₃ C(═O)cyclopropyl H O 0 A-2560 H H H H H CH₂CH₂SOCF₃ C(═O)cyclopropyl H O 0 A-2561 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)cyclopropyl H O 0 A-2562 H H H H H CH₂SO₂CF₃ C(═O)cyclopropyl H O 0 A-2563 H H H H H CH₂CH₂SO₂CF₃ C(═O)cyclopropyl H O 0 A-2564 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)cyclopropyl H O 0 A-2565 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)cyclopropyl H O 0 A-2566 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)cyclopropyl H O 0 A-2567 H H H H H H C(═O)OCH₃ H O 0 A-2568 H H H H H CH₃ C(═O)OCH₃ H O 0 A-2569 H H H H H CH₂CH₃ C(═O)OCH₃ H O 0 A-2570 H H H H H CH(CH₃)₂ C(═O)OCH₃ H O 0 A-2571 H H H H H CH₂CH₂CH₃ C(═O)OCH₃ H O 0 A-2572 H H H H H CH₂CH(CH₃)₂ C(═O)OCH₃ H O 0 A-2573 H H H H H CH₂C(CH₃)₃ C(═O)OCH₃ H O 0 A-2574 H H H H H CH(CH₃)CH₂CH₃ C(═O)OCH₃ H O 0 A-2575 H H H H H CH₂(CH₂)₂CH₃ C(═O)OCH₃ H O 0 A-2576 H H H H H CH₂(CH₂)₃CH₃ C(═O)OCH₃ H O 0 A-2577 H H H H H CH₂(CH₂)₄CH₃ C(═O)OCH₃ H O 0 A-2578 H H H H H CHACH₂)₆CH₃ C(═O)OCH₃ H O 0 A-2579 H H H H H CH₂OCH₃ C(═O)OCH₃ H O 0 A-2580 H H H H H CH₂OCH₂CH₃ C(═O)OCH₃ H O 0 A-2581 H H H H H CH₂CH₂OCH₃ C(═O)OCH₃ H O 0 A-2582 H H H H H CH₂CH₂OCH₂CH₃ C(═O)OCH₃ H O 0 A-2583 H H H H H CF₃ C(═O)OCH₃ H O 0 A-2584 H H H H H CHF₂ C(═O)OCH₃ H O 0 A-2585 H H H H H CH₂CF₃ C(═O)OCH₃ H O 0 A-2586 H H H H H CH₂CHF₂ C(═O)OCH₃ H O 0 A-2587 H H H H H CH₂CClF₂ C(═O)OCH₃ H O 0 A-2588 H H H H H CH₂CBrF₂ C(═O)OCH₃ H O 0 A-2589 H H H H H CF₂CF₃ C(═O)OCH₃ H O 0 A-2590 H H H H H CF₂CHF₂ C(═O)OCH₃ H O 0 A-2591 H H H H H CH₂CH₂CF₃ C(═O)OCH₃ H O 0 A-2592 H H H H H CH₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2593 H H H H H CH₂CF₂CHF₂ C(═O)OCH₃ H O 0 A-2594 H H H H H CF₂CHFCF₃ C(═O)OCH₃ H O 0 A-2595 H H H H H CF₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2596 H H H H H CH₂CF₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2597 H H H H H CH₂CF₂CHFCF₃ C(═O)OCH₃ H O 0 A-2598 H H H H H CH₂CH₂CH₂CF₃ C(═O)OCH₃ H O 0 A-2599 H H H H H CH₂CH₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2600 H H H H H CF₂CF₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2601 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)OCH₃ H O 0 A-2602 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2603 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2604 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)OCH₃ H O 0 A-2605 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)OCH₃ H O 0 A-2606 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ C(═O)OCH₃ H O 0 A-2607 H H H H H CF₂CHFOCH₃ C(═O)OCH₃ H O 0 A-2608 H H H H H CF₂CHFOCH₂CH₃ C(═O)OCH₃ H O 0 A-2609 H H H H H CH₂CH₂OCH₂CF₃ C(═O)OCH₃ H O 0 A-2610 H H H H H CF₂CHFOCF₃ C(═O)OCH₃ H O 0 A-2611 H H H H H CF₂CHFOCF₂CF₃ C(═O)OCH₃ H O 0 A-2612 H H H H H CF₂CHFOCF₂CF₂CF₃ C(═O)OCH₃ H O 0 A-2613 H H H H H CH₂CH═CH₂ C(═O)OCH₃ H O 0 A-2614 H H H H H CH₂CH═CHCl C(═O)OCH₃ H O 0 A-2615 H H H H H CH₂CH═CCl₂ C(═O)OCH₃ H O 0 A-2616 H H H H H CH₂CH₂CF═CF₂ C(═O)OCH₃ H O 0 A-2617 H H H H H CH₂CH₂CH═CF₂ C(═O)OCH₃ H O 0 A-2618 H H H H H CH₂C≡CH C(═O)OCH₃ H O 0

TABLE 44 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2619 H H H H H CH₂C≡CCH₃ C(═O)OCH₃ H O 0 A-2620 H H H H H CH₂C≡CI C(═O)OCH₃ H O 0 A-2621 H H H H H CH₂C≡CCF₃ C(═O)OCH₃ H O 0 A-2622 H H H H H cyclobutyl C(═O)OCH₃ H O 0 A-2623 H H H H H cyclopentyl C(═O)OCH₃ H O 0 A-2624 H H H H H cyclohexyl C(═O)OCH₃ H O 0 A-2625 H H H H H 4,4-difluorocyclohexyl C(═O)OCH₃ H O 0 A-2626 H H H H H CH₂(cyclopropyl) C(═O)OCH₃ H O 0 A-2627 H H H H H CH₂(cyclobutyl) C(═O)OCH₃ H O 0 A-2628 H H H H H CH₂(cyclopentyl) C(═O)OCH₃ H O 0 A-2629 H H H H H CH₂CH₂(cyclopropyl) C(═O)OCH₃ H O 0 A-2630 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)OCH₃ H O 0 A-2631 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)OCH₃ H O 0 A-2632 H H H H H CH₂(4,4-difluorocyclohexyl) C(═O)OCH₃ H O 0 A-2633 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)OCH₃ H O 0 A-2634 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)OCH₃ H O 0 A-2635 H H H H H CH₂SCH₃ C(═O)OCH₃ H O 0 A-2636 H H H H H CH₂SCH₂CH₃ C(═O)OCH₃ H O 0 A-2637 H H H H H CH₂CH₂SCH₃ C(═O)OCH₃ H O 0 A-2638 H H H H H CH₂CH₂SCH₂CH₃ C(═O)OCH₃ H O 0 A-2639 H H H H H CH₂CH₂CH₂SCH₃ C(═O)OCH₃ H O 0 A-2640 H H H H H CH₂CH₂CH₂SCH₂CH₃ C(═O)OCH₃ H O 0 A-2641 H H H H H CH(CH₃)SCH₃ C(═O)OCH₃ H O 0 A-2642 H H H H H CH(CH₃)SCH₂CH₃ C(═O)OCH₃ H O 0 A-2643 H H H H H CH₂CH(CH₃)SCH₃ C(═O)OCH₃ H O 0 A-2644 H H H H H CH₂CH(CH₃)SCH₂CH₃ C(═O)OCH₃ H O 0 A-2645 H H H H H CH(CH₃)CH₂CH₂SCH₃ C(═O)OCH₃ H O 0 A-2646 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ C(═O)OCH₃ H O 0 A-2647 H H H H H CH₂CH(CH₃)CH₂SCH₃ C(═O)OCH₃ H O 0 A-2648 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ C(═O)OCH₃ H O 0 A-2649 H H H H H CH₂CH₂CH(CH₃)SCH₃ C(═O)OCH₃ H O 0 A-2650 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ C(═O)OCH₃ H O 0 A-2651 H H H H H CH₂SOCH₃ C(═O)OCH₃ H O 0 A-2652 H H H H H CH₂CH₂SOCH₃ C(═O)OCH₃ H O 0 A-2653 H H H H H CH₂CH₂CH₂SOCH₃ C(═O)OCH₃ H O 0 A-2654 H H H H H CH(CH₃)SOCH₃ C(═O)OCH₃ H O 0 A-2655 H H H H H CH₂CH(CH₃)SOCH₃ C(═O)OCH₃ H O 0 A-2656 H H H H H CH(CH₃)CH₂CH₂SOCH₃ C(═O)OCH₃ H O 0 A-2657 H H H H H CH₂CH(CH₃)CH₂SOCH₃ C(═O)OCH₃ H O 0 A-2658 H H H H H CH₂CH₂CH(CH₃)SOCH₃ C(═O)OCH₃ H O 0 A-2659 H H H H H CH₂SO₂CH₃ C(═O)OCH₃ H O 0 A-2660 H H H II H CH₂CH₂SO₂CH₃ C(═O)OCH₃ H O 0 A-2661 H H H H H CH₂CH₂CH₂SO₂CH₃ C(═O)OCH₃ H O 0 A-2662 H H H H H CH(CH₃)SO₂CH₃ C(═O)OCH₃ H O 0 A-2663 H H H H H CH₂CH(CH₃)SO₂CH₃ C(═O)OCH₃ H O 0 A-2664 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ C(═O)OCH₃ H O 0 A-2665 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ C(═O)OCH₃ H O 0 A-2666 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ C(═O)OCH₃ H O 0 A-2667 H H H H H CH₂SCF₃ C(═O)OCH₃ H O 0 A-2668 H H H H H CH₂SCHF₂ C(═O)OCH₃ H O 0 A-2669 H H H H H CH₂SCH₂CF₃ C(═O)OCH₃ H O 0 A-2670 H H H H H CH₂SCH₂CHF₂ C(═O)OCH₃ H O 0 A-2671 H H H H H CH₂SCF₂CF₃ C(═O)OCH₃ H O 0 A-2672 H H H H H CH₂CH₂SCF₃ C(═O)OCH₃ H O 0 A-2673 H H H H H CH₂CH₂SCH₂CF₃ C(═O)OCH₃ H O 0 A-2674 H H H H H CH₂CH₂CH₂SCF₃ C(═O)OCH₃ H O 0 A-2675 H H H H H CH₂CH₂CH₂SCH₂CF₃ C(═O)OCH₃ H O 0 A-2676 H H H H H CH(CH₃)SCF₃ C(═O)OCH₃ H O 0 A-2677 H H H H H CH(CH₃)SCH₂CF₃ C(═O)OCH₃ H O 0 A-2678 H H H H H CH₂CH(CH₃)SCF₃ C(═O)OCH₃ H O 0 A-2679 H H H H H CH₂CH(CH₃)SCH₂CF₃ C(═O)OCH₃ H O 0

TABLE 45 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2680 H H H H H CH(CH₃)CH₂CH₂SCF₃ C(═O)OCH₃ H O 0 A-2681 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ C(═O)OCH₃ H O 0 A-2682 H H H H H CH₂CH(CH₃)CH₂SCF₃ C(═O)OCH₃ H O 0 A-2683 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ C(═O)OCH₃ H O 0 A-2684 H H H H H CH₂CH₂CH(CH₃)SCF₃ C(═O)OCH₃ H O 0 A-2685 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ C(═O)OCH₃ H O 0 A-2686 H H H H H CH₂SOCF₃ C(═O)OCH₃ H O 0 A-2687 H H H H H CH₂CH₂SOCF₃ C(═O)OCH₃ H O 0 A-2688 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)OCH₃ H O 0 A-2689 H H H H H CH(CH₃)SOCF₃ C(═O)OCH₃ H O 0 A-2690 H H H H H CH₂CH(CH₃)SOCF₃ C(═O)OCH₃ H O 0 A-2691 H H H H H CH(CH₃)CH₂CH₂SOCF₃ C(═O)OCH₃ H O 0 A-2692 H H H H H CH₂CH(CH₃)CH₂SOCF₃ C(═O)OCH₃ H O 0 A-2693 H H H H H CH₂CH₂CH(CH₃)SOCF₃ C(═O)OCH₃ H O 0 A-2694 H H H H H CH₂SO₂CF₃ C(═O)OCH₃ H O 0 A-2695 H H H H H CH₂CH₂SO₂CF₃ C(═O)OCH₃ H O 0 A-2696 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)OCH₃ H O 0 A-2697 H H H H H CH(CH₃)SO₂CF₃ C(═O)OCH₃ H O 0 A-2698 H H H H H CH₂CH(CH₃)SO₂CF₃ C(═O)OCH₃ H O 0 A-2699 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ C(═O)OCH₃ H O 0 A-2700 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ C(═O)OCH₃ H O 0 A-2701 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ C(═O)OCH₃ H O 0 A-2702 H H H H H CH₂C(═O)CH₃ C(═O)OCH₃ H O 0 A-2703 H H H H H CH₂C(═O)CH₂CH₃ C(═O)OCH₃ H O 0 A-2704 H H H H H CH₂C(═O)C(CH₃)₃ C(═O)OCH₃ H O 0 A-2705 H H H H H CH₂CH₂C(═O)CH₃ C(═O)OCH₃ H O 0 A-2706 H H H H H CH₂CH₂C(═O)C(CH₃)₃ C(═O)OCH₃ H O 0 A-2707 H H H H H CH₂C(═O)CF₃ C(═O)OCH₃ H O 0 A-2708 H H H H H CH₂CH₂C(═O)CF₃ C(═O)OCH₃ H O 0 A-2709 H H H H H CH₂C(═O)OCH₃ C(═O)OCH₃ H O 0 A-2710 H H H H H CH₂C(═O)OCH₂CH₃ C(═O)OCH₃ H O 0 A-2711 H H H H H CH₂C(═O)OC(CH₃)₃ C(═O)OCH₃ H O 0 A-2712 H H H H H CH₂CH₂C(═O)OCH₃ C(═O)OCH₃ H O 0 A-2713 H H H H H CH₂CH₂C(═O)OCH₂CH₃ C(═O)OCH₃ H O 0 A-2714 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ C(═O)OCH₃ H O 0 A-2715 H H H H H CH₂C(═O)NH₂ C(═O)OCH₃ H O 0 A-2716 H H H H H CH₂CH₂C(═O)NH₂ C(═O)OCH₃ H O 0 A-2717 H H H H H CH₂C(═O)NHCH₃ C(═O)OCH₃ H O 0 A-2718 H H H H H CH₂C(═O)NHCH(CH₃)₂ C(═O)OCH₃ H O 0 A-2719 H H H H H CH₂CH₂C(═O)NHCH₃ C(═O)OCH₃ H O 0 A-2720 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ C(═O)OCH₃ H O 0 A-2721 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)OCH₃ H O 0 A-2722 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)OCH₃ H O 0 A-2723 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ C(═O)OCH₃ H O 0 A-2724 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ C(═O)OCH₃ H O 0 A-2725 H H H H H CH₂C(═O)N(CH₃)₂ C(═O)OCH₃ H O 0 A-2726 H H H H H CH₂C(═O)N(CH₂CH₃)₂ C(═O)OCH₃ H O 0 A-2727 H H H H H CH₂CH₂C(═O)N(CH₃)₂ C(═O)OCH₃ H O 0 A-2728 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ C(═O)OCH₃ H O 0 A-2729 H H H H H CH₂CH₂OH C(═O)OCH₃ H O 0 A-2730 H H H H H CH₂CH(OH)CH₃ C(═O)OCH₃ H O 0 A-2731 H H H H H CH₂CH₂CH₂OH C(═O)OCH₃ H O 0 A-2732 H H H H H CH₂CH(OH)CH₂CH₃ C(═O)OCH₃ H O 0 A-2733 H H H H H CH₂CH(OH)C(CH₃)₃ C(═O)OCH₃ H O 0 A-2734 H H H H H CH₂CH₂CH(OH)CH₃ C(═O)OCH₃ H O 0 A-2735 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ C(═O)OCH₃ H O 0 A-2736 H H H H H CH₂C(═NOH)CH₃ C(═O)OCH₃ H O 0 A-2737 H H H H H CH₂C(═NOH)CH₂CH₃ C(═O)OCH₃ H O 0 A-2738 H H H H H CH₂C(═NOH)C(CH₃)₃ C(═O)OCH₃ H O 0 A-2739 H H H H H CH₂C(═NOCH₃)CH₃ C(═O)OCH₃ H O 0 A-2740 H H H H H CH₂C(═NOCH₃)CH₂CH₃ C(═O)OCH₃ H O 0

TABLE 46 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2741 H H H H H CH₂C(═NOCH₂CH₃)CH₃ C(═O)OCH₃ H O 0 A-2742 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ C(═O)OCH₃ H O 0 A-2743 H H H H H CH₂C(═NOCH₂CF₃)CH₃ C(═O)OCH₃ H O 0 A-2744 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ C(═O)OCH₃ H O 0 A-2745 H H H H H CH₂Ph C(═O)OCH₃ H O 0 A-2746 H H H H H CH₂(2-F)Ph C(═O)OCH₃ H O 0 A-2747 H H H H H CH₂(3-F)Ph C(═O)OCH₃ H O 0 A-2748 H H H H H CH₂(4-F)Ph C(═O)OCH₃ H O 0 A-2749 H H H H H CH₂(2-Cl)Ph C(═O)OCH₃ H O 0 A-2750 H H H H H CH₂(3-Cl)Ph C(═O)OCH₃ H O 0 A-2751 H H H H H CH₂(4-Cl)Ph C(═O)OCH₃ H O 0 A-2752 H H H H H CH₂(2-CF₃)Ph C(═O)OCH₃ H O 0 A-2753 H H H H H CH₂(3-CF₃)Ph C(═O)OCH₃ H O 0 A-2754 H H H H H CH₂(4-CF₃)Ph C(═O)OCH₃ H O 0 A-2755 H H H H H CH₂(naphthalen-1-yl) C(═O)OCH₃ H O 0 A-2756 H H H H H CH₂(naphthalen-2-yl) C(═O)OCH₃ H O 0 A-2757 H H H H H CH₂CH₂Ph C(═O)OCH₃ H O 0 A-2758 H H H H H H C(═O)OCH₂CH₃ H O 0 A-2759 H H H H H CH₃ C(═O)OCH₂CH₃ H O 0 A-2760 H H H H H CH₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2761 H H H H H CH(CH₃)₂ C(═O)OCH₂CH₃ H O 0 A-2762 H H H H H CH₂CH₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2763 H H H H H CH₂CH(CH₃)₂ C(═O)OCH₂CH₃ H O 0 A-2764 H H H H H CH(CH₃)CH₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2765 H H H H H CH₂C(CH₃)₃ C(═O)OCH₂CH₃ H O 0 A-2766 H H H H H CH₂(CH₂)₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2767 H H H H H CH₂(CH₂)₃CH₃ C(═O)OCH₂CH₃ H O 0 A-2768 H H H H H CF₃ C(═O)OCH₂CH₃ H O 0 A-2769 H H H H H CHF₂ C(═O)OCH₂CH₃ H O 0 A-2770 H H H H H CH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2771 H H H H H CH₂CHF₂ C(═O)OCH₂CH₃ H O 0 A-2772 H H H H H CH₂CCIF₂ C(═O)OCH₂CH₃ H O 0 A-2773 H H H H H CH₂CBrF₂ C(═O)OCH₂CH₃ H O 0 A-2774 H H H H H CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2775 H H H H H CF₂CHF₂ C(═O)OCH₂CH₃ H O 0 A-2776 H H H H H CH₂CH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2777 H H H H H CH₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2778 H H H H H CH₂CF₂CHF₂ C(═O)OCH₂CH₃ H O 0 A-2779 H H H H H CF₂CHFCF₃ C(═O)OCH₂CH₃ H O 0 A-2780 H H H H H CF₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2781 H H H H H CH₂CF₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2782 H H H H H CH₂CF₂CHFCF₃ C(═O)OCH₂CH₃ H O 0 A-2783 H H H H H CH₂CH₂CH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2784 H H H H H CH₂CH₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2785 H H H H H CF₂CF₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2786 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)OCH₂CH₃ H O 0 A-2787 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2788 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2789 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2790 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)OCH₂CH₃ H O 0 A-2791 H H H H H CH₂CH₂OCH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2792 H H H H H CF₂CHFOCF₃ C(═O)OCH₂CH₃ H O 0 A-2793 H H H H H CF₂CHFOCF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2794 H H H H H CH₂CH₂CF═CF₂ C(═O)OCH₂CH₃ H O 0 A-2795 H H H H H CH₂CH₂CH═CF₂ C(═O)OCH₂CH₃ H O 0 A-2796 H H H H H CH₂C≡CCH₃ C(═O)OCH₂CH₃ H O 0 A-2797 H H H H H CH₂C≡CCF₃ C(═O)OCH₂CH₃ H O 0 A-2798 H H H H H CH₂C≡CI C(═O)OCH₂CH₃ H O 0 A-2799 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)OCH₂CH₃ H O 0 A-2800 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)OCH₂CH₃ H O 0 A-2801 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)OCH₂CH₃ H O 0

TABLE 47 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2802 H H H H H CH₂CH₂(2,2- C(═O)OCH₂CH₃ H O 0 dichlorocyclopropyl) A-2803 H H H H H CH₂SCH₃ C(═O)OCH₂CH₃ H O 0 A-2804 H H H H H CH₂SCH₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2805 H H H H H CH₂CH₂SCH₃ C(═O)OCH₂CH₃ H O 0 A-2806 H H H H H CH₂SOCH₃ C(═O)OCH₂CH₃ H O 0 A-2807 H H H H H CH₂CH₂SOCH₃ C(═O)OCH₂CH₃ H O 0 A-2808 H H H H H CH₂SO₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2809 H H H H H CH₂CH₂SO₂CH₃ C(═O)OCH₂CH₃ H O 0 A-2810 H H H H H CH₂SCF₃ C(═O)OCH₂CH₃ H O 0 A-2811 H H H H H CH₂SCHF₂ C(═O)OCH₂CH₃ H O 0 A-2812 H H H H H CH₂SCH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2813 H H H H H CH₂SCH₂CHF₃ C(═O)OCH₂CH₃ H O 0 A-2814 H H H H H CH₂SCF₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2815 H H H H H CH₂CH₂SCF₃ C(═O)OCH₂CH₃ H O 0 A-2816 H H H H H CH₂SOCF₃ C(═O)OCH₂CH₃ H O 0 A-2817 H H H H H CH₂CH₂SOCF₃ C(═O)OCH₂CH₃ H O 0 A-2818 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)OCH₂CH₃ H O 0 A-2819 H H H H H CH₂SO₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2820 H H H H H CH₂CH₂SO₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2821 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2822 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)OCH₂CH₃ H O 0 A-2823 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)OCH₂CH₃ H O 0 A-2824 H H H H H H C(═O)OCH(CH₃)₂ H O 0 A-2825 H H H H H CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2826 H H H H H CH₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2827 H H H H H CH(CH₃)₂ C(═O)OCH(CH₃)₂ H O 0 A-2828 H H H H H CH₂CH₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2829 H H H H H CH₂CH(CH₃)₂ C(═O)OCH(CH₃)₂ H O 0 A-2830 H H H H H CH(CH₃)CH₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2831 H H H H H CH₂C(CH₃)₃ C(═O)OCH(CH₃)₂ H O 0 A-2832 H H H H H CH₂(CH₂)₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2833 H H H H H CH₂(CH₂)₃CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2834 H H H H H CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2835 H H H H H CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2836 H H H H H CH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2837 H H H H H CH₂CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2838 H H H H H CH₂CCIF₂ C(═O)OCH(CH₃)₂ H O 0 A-2839 H H H H H CH₂CBrF₂ C(═O)OCH(CH₃)₂ H O 0 A-2840 H H H H H CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2841 H H H H H CF₂CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2842 H H H H H CH₂CH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2843 H H H H H CH₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2044 H H H H H CH₂CF₂CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2845 H H H H H CF₂CHFCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2846 H H H H H CF₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2847 H H H H H CH₂CF₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2848 H H H H H CH₂CF₂CHFCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2849 H H H H H CH₂CH₂CH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2850 H H H H H CH₂CH₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2851 H H H H H CF₂CF₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2852 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)OCH(CH₃)₂ H O 0 A-2853 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2854 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2855 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2856 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2857 H H H H H CH₂CH₂OCH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2858 H H H H H CF₂CHFOCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2859 H H H H H CF₂CHFOCF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2860 H H H H H CH₂CH₂CF═CF₂ C(═O)OCH(CH₃)₂ H O 0 A-2861 H H H H H CH₂CH₂CH═CF₂ C(═O)OCH(CH₃)₂ H O 0 A-2862 H H H H H CH₂C≡CCH₃ C(═O)OCH(CH₃)₂ H O 0

TABLE 48 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2863 H H H H H CH₂C≡CCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2864 H H H H H CH₂C≡CI C(═O)OCH(CH₃)₂ H O 0 A-2865 H H H H H CH₂(2,2- C(═O)OCH(CH₃)₂ H O 0 difluorecyclopropyl) A-2866 H H H H H CH₂(2,2- C(═O)OCH(CH₃)₂ H O 0 dichlorocyclopropyl) A-2867 H H H H H CH₂CH₂(2,2- C(═O)OCH(CH₃)₂ H O 0 difluorocyclopropyl) A-2868 H H H H H CH₂CH₂(2,2- C(═O)OCH(CH₃)₂ H O 0 dichlorocyclopropyl) A-2869 H H H H H CH₂SCH₃ C(═O)OCH(CH₃)₂ H O 0 A-2870 H H H H H CH₂SCH₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2871 H H H H H CH₂CH₂SCH₃ C(═O)OCH(CH₃)₂ H O 0 A-2872 H H H H H CH₂SOCH₃ C(═O)OCH(CH₃)₂ H O 0 A-2873 H H H H H CH₂CH₂SOCH₃ C(═O)OCH(CH₃)₂ H O 0 A-2874 H H H H H CH₂SO₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2875 H H H H H CH₂CH₂SO₂CH₃ C(═O)OCH(CH₃)₂ H O 0 A-2876 H H H H H CH₂SCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2877 H H H H H CH₂SCHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2878 H H H H H CH₂SCH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2879 H H H H H CH₂SCH₂CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2880 H H H H H CH₂SCF₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2881 H H H H H CH₂CH₂SCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2882 H H H H H CH₂SOCF₂ C(═O)OCH(CH₃)₂ H O 0 A-2883 H H H H H CH₂CH₂SOCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2884 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)OCH(CH₃)₂ H O 0 A-2885 H H H H H CH₂SO₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2886 H H H H H CH₂CH₂SO₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2887 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2888 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)OCH(CH₃)₂ H O 0 A-2889 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)OCH(CH₃)₂ H O 0 A-2890 H H H H H H C(═O)N(CH₃)₂ H O 0 A-2891 H H H H H CH₃ C(═O)N(CH₃)₂ H O 0 A-2892 H H H H H CH₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2893 H H H H H CH(CH₃)₂ C(═O)N(CH₃)₂ H O 0 A-2894 H H H H H CH₂CH₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2895 H H H H H CH₂CH(CH₃)₂ C(═O)N(CH₃)₂ H O 0 A-2896 H H H H H CH(CH₃)CH₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2897 H H H H H CH₂C(CH₃)₃ C(═O)N(CH₃)₂ H O 0 A-2898 H H H H H CH₂(CH₂)₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2899 H H H H H CH₂(CH₂)₃CH₃ C(═O)N(CH₃)₂ H O 0 A-2900 H H H H H CF₃ C(═O)N(CH₃)₂ H O 0 A-2901 H H H H H CHF₂ C(═O)N(CH₃)₂ H O 0 A-2902 H H H H H CH₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2903 H H H H H CH₂CHF₂ C(═O)N(CH₃)₂ H O 0 A-2904 H H H H H CH₂CCIF₂ C(═O)N(CH₃)₂ H O 0 A-2905 H H H H H CH₂CBrF₂ C(═O)N(CH₃)₂ H O 0 A-2906 H H H H H CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2907 H H H H H CF₂CHF₂ C(═O)N(CH₃)₂ H O 0 A-2908 H H H H H CH₂CH₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2909 H H H H H CH₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2910 H H H H H CH₂CF₂CHF₂ C(═O)N(CH₃)₂ H O 0 A-2911 H H H H H CF₂CHFCF₃ C(═O)N(CH₃)₂ H O 0 A-2912 H H H H H CF₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2913 H H H H H CH₂CF₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2914 H H H H H CH₂CF₂CHFCF₃ C(═O)N(CH₃)₂ H O 0 A-2915 H H H H H CH₂CH₂CH₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2916 H H H H H CH₂CH₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2917 H H H H H CF₂CF₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2918 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)N(CH₃)₂ H O 0 A-2919 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2920 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2921 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2922 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)N(CH₃)₂ H O 0 A-2923 H H H H H CH₂CH₂OCH₂CF₃ C(═O)N(CH₃)₂ H O 0

TABLE 49 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2924 H H H H H CF₂CHFOCF₃ C(═O)N(CH₃)₂ H O 0 A-2925 H H H H H CF₂CHFOCF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2926 H H H H H CH₂CH₂CF═CF₂ C(═O)N(CH₃)₂ H O 0 A-2927 H H H H H CH₂CH₂CH═CF₂ C(═O)N(CH₃)₂ H O 0 A-2928 H H H H H CH₂C≡CCH₃ C(═O)N(CH₃)₂ H O 0 A-2929 H H H H H CH₂C≡CCF₃ C(═O)N(CH₃)₂ H O 0 A-2930 H H H H H CH₂C≡CI C(═O)N(CH₃)₂ H O 0 A-2931 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)N(CH₃)₂ H O 0 A-2932 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)N(CH₃)₂ H O 0 A-2933 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)N(CH₃)₂ H O 0 A-2934 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)N(CH₃)₂ H O 0 A-2935 H H H H H CH₂SCH₃ C(═O)N(CH₃)₂ H O 0 A-2936 H H H H H CH₂SCH₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2937 H H H H H CH₂CH₂SCH₃ C(═O)N(CH₃)₂ H O 0 A-2938 H H H H H CH₂SOCH₃ C(═O)N(CH₃)₂ H O 0 A-2939 H H H H H CH₂CH₂SOCH₃ C(═O)N(CH₃)₂ H O 0 A-2940 H H H H H CH₂SO₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2941 H H H H H CH₂CH₂SO₂CH₃ C(═O)N(CH₃)₂ H O 0 A-2942 H H H H H CH₂SCF₃ C(═O)N(CH₃)₂ H O 0 A-2943 H H H H H CH₂SCHF₂ C(═O)N(CH₃)₂ H O 0 A-2944 H H H H H CH₂SCH₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2945 H H H H H CH₂SCH₂CHF₂ C(═O)N(CH₃)₂ H O 0 A-2946 H H H H H CH₂SCF₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2947 H H H H H CH₂CH₂SCF₃ C(═O)N(CH₃)₂ H O 0 A-2948 H H H H H CH₂SOCF₃ C(═O)N(CH₃)₂ H O 0 A-2949 H H H H H CH₂CH₂SOCF₃ C(═O)N(CH₃)₂ H O 0 A-2950 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)N(CH₃)₂ H O 0 A-2951 H H H H H CH₂SO₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2952 H H H H H CH₂CH₂SO₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2953 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2954 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)N(CH₃)₂ H O 0 A-2955 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)N(CH₃)₂ H O 0 A-2956 H H H H H H C(═O)(4-Cl)Ph H O 0 A-2957 H H H H H CH₃ C(═O)(4-Cl)Ph H O 0 A-2958 H H H H H CH₂CH₃ C(═O)(4-Cl)Ph H O 0 A-2959 H H H H H CH(CH₃)₂ C(═O)(4-Cl)Ph H O 0 A-2960 H H H H H CH₂CH₂CH₃ C(═O)(4-Cl)Ph H O 0 A-2961 H H H H H CH₂CH(CH₃)₂ C(═O)(4-Cl)Ph H O 0 A-2962 H H H H H CH(CH₂)CH₂CH₃ C(═O)(4-Cl)Ph H O 0 A-2963 H H H H H CH₂C(CH₃)₃ C(═O)(4-Cl)Ph H O 0 A-2964 H H H H H CH₂(CH₂)₂CH₃ C(═O)(4-Cl)Ph H O 0 A-2965 H H H H H CH₂(CH₂)₃CH₃ C(═O)(4-Cl)Ph H O 0 A-2966 H H H H H CF₃ C(═O)(4-Cl)Ph H O 0 A-2967 H H H H H CHF₂ C(═O)(4-Cl)Ph H O 0 A-2968 H H H H H CH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2969 H H H H H CH₂CHF₂ C(═O)(4-Cl)Ph H O 0 A-2970 H H H H H CH₂CCIF₂ C(═O)(4-Cl)Ph H O 0 A-2971 H H H H H CH₂CBrF₂ C(═O)(4-Cl)Ph H O 0 A-2972 H H H H H CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2973 H H H H H CF₂CHF₂ C(═O)(4-Cl)Ph H O 0 A-2974 H H H H H CH₂CH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2975 H H H H H CH₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2976 H H H H H CH₂CF₂CHF₂ C(═O)(4-Cl)Ph H O 0 A-2977 H H H H H CF₂CHFCF₃ C(═O)(4-Cl)Ph H O 0 A-2978 H H H H H CF₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2979 H H H H H CH₂CF₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2980 H H H H H CH₂CF₂CHFCF₃ C(═O)(4-Cl)Ph H O 0 A-2981 H H H H H CH₂CH₂CH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2982 H H H H H CH₂CH₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2983 H H H H H CF₂CF₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2984 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)(4-Cl)Ph H O 0

TABLE 50 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-2985 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2986 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2987 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2988 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)(4-Cl)Ph H O 0 A-2989 H H H H H CH₂CH₂OCH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2990 H H H H H CF₂CHFOCF₃ C(═O)(4-Cl)Ph H O 0 A-2991 H H H H H CF₂CHFOCF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-2992 H H H H H CH₂CH₂CF═CF₂ C(═O)(4-Cl)Ph H O 0 A-2993 H H H H H CH₂CH₂CH═CF₂ C(═O)(4-Cl)Ph H O 0 A-2994 H H H H H CH₂C≡CCH₃ C(═O)(4-Cl)Ph H O 0 A-2995 H H H H H CH₂C≡CCF₃ C(═O)(4-Cl)Ph H O 0 A-2996 H H H H H CH₂C≡CI C(═O)(4-Cl)Ph H O 0 A-2997 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)(4-Cl)Ph H O 0 A-2998 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)(4-Cl)Ph H O 0 A-2999 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)(4-Cl)Ph H O 0 A-3000 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)(4-Cl)Ph H O 0 A-3001 H H H H H CH₂SCH₃ C(═O)(4-Cl)Ph H O 0 A-3002 H H H H H CH₂SCH₂CH₃ C(═O)(4-Cl)Ph H O 0 A-3003 H H H H H CH₂CH₂SCH₃ C(═O)(4-Cl)Ph H O 0 A-3004 H H H H H CH₂SOCH₃ C(═O)(4-Cl)Ph H O 0 A-3005 H H H H H CH₂CH₂SOCH₃ C(═O)(4-Cl)Ph H O 0 A-3006 H H H H H CH₂SO₂CH₃ C(═O)(4-Cl)Ph H O 0 A-3007 H H H H H CH₂CH₂SO₂CH₃ C(═O)(4-Cl)Ph H O 0 A-3008 H H H H H CH₂SCF₃ C(═O)(4-Cl)Ph H O 0 A-3009 H H H H H CH₂SCHF₂ C(═O)(4-Cl)Ph H O 0 A-3010 H H H H H CH₂SCH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-3011 H H H H H CH₂SCH₂CHF₂ C(═O)(4-Cl)Ph H O 0 A-3012 H H H H H CH₂SCF₂CF₃ C(═O)(4-Cl)Ph H O 0 A-3013 H H H H H CH₂CH₂SCF₃ C(═O)(4-Cl)Ph H O 0 A-3014 H H H H H CH₂SOCF₃ C(═O)(4-Cl)Ph H O 0 A-3015 H H H H H CH₂CH₂SOCF₃ C(═O)(4-Cl)Ph H O 0 A-3016 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)(4-Cl)Ph H O 0 A-3017 H H H H H CH₂SO₂CF₃ C(═O)(4-Cl)Ph H O 0 A-3018 H H H H H CH₂CH₂SO₂CF₃ C(═O)(4-Cl)Ph H O 0 A-3019 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)(4-Cl)Ph H O 0 A-3020 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)(4-Cl)Ph H O 0 A-3021 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)(4-Cl)Ph H O 0 A-3022 H H H H H H C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3023 H H H H H CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3024 H H H H H CH₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3025 H H H H H CH(CH₃)₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3026 H H H H H CH₂CH₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3027 H H H H H CH₂CH(CH₃)₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3028 H H H H H CH(CH₃)CH₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3029 H H H H H CH₂C(CH₃)₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3030 H H H H H CH₂(CH₂)₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3031 H H H H H CH₂(CH₂)₃CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3032 H H H H H CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3033 H H H H H CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3034 H H H H H CH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3035 H H H H H CH₂CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3036 H H H H H CH₂CCIF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3037 H H H H H CH₂CBrF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3038 H H H H H CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3039 H H H H H CF₂CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3040 H H H H H CH₂CH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3041 H H H H H CH₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3042 H H H H H CH₂CF₂CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3043 H H H H H CF₂CHFCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3044 H H H H H CF₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3045 H H H H H CH₂CF₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0

TABLE 51 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3046 H H H H H CH₂CF₂CHFCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3047 H H H H H CH₂CH₂CH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3048 H H H H H CH₂CH₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3049 H H H H H CF₂CF₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3050 H H H H H CH₂CH₂CH(CF₃)₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3051 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3052 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3053 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3054 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3055 H H H H H CH₂CH₂OCH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3056 H H H H H CF₂CHFOCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3057 H H H H H CF₂CHFOCF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3058 H H H H H CH₂CH₂CF═CF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3059 H H H H H CH₂CH₂CH═CF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3060 H H H H H CH₂C≡CCH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3061 H H H H H CH₂C≡CCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3062 H H H H H CH₂C≡CI C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3063 H H H H H CH₂(2,2-difluorocyclopropyl) C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3064 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3065 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3066 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3067 H H H H H CH₂SCH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3068 H H H H H CH₂SCH₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3069 H H H H H CH₂CH₂SCH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3070 H H H H H CH₂SOCH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3071 H H H H H CH₂CH₂SOCH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3072 H H H H H CH₂SO₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3073 H H H H H CH₂CH₂SO₂CH₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3074 H H H H H CH₂SCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3075 H H H H H CH₂SCHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3076 H H H H H CH₂SCH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3077 H H H H H CH₂SCH₂CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3078 H H H H H CH₂SCF₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3079 H H H H H CH₂CH₂SCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3080 H H H H H CH₂SOCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3081 H H H H H CH₂CH₂SOCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3082 H H H H H CH₂CH₂CH₂SOCF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3083 H H H H H CH₂SO₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3084 H H H H H CH₂CH₂SO₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3085 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3086 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3087 H H H H H CH₂C(═O)NHCH₂CF₃ C(═O)(2,6-Cl₂)pyridin-4-yl H O 0 A-3088 H H H H H H C(═S)OCH₃ H O 0 A-3089 H H H H H CH₃ C(═S)OCH₃ H O 0 A-3090 H H H H H CH₂CH₃ C(═S)OCH₃ H O 0 A-3091 H H H H H CH(CH₃)₂ C(═S)OCH₃ H O 0 A-3092 H H H H H CH₂CH₂CH₃ C(═S)OCH₃ H O 0 A-3093 H H H H H CH₂CH(CH₃)₂ C(═S)OCH₃ H O 0 A-3094 H H H H H CH(CH₃)CH₂CH₃ C(═S)OCH₃ H O 0 A-3095 H H H H H CH₂C(CH₃)₃ C(═S)OCH₃ H O 0 A-3096 H H H H H CH₂(CH₂)₂CH₃ C(═S)OCH₃ H O 0 A-3097 H H H H H CH₂(CH₂)₃CH₃ C(═S)OCH₃ H O 0 A-3098 H H H H H CF₃ C(═S)OCH₃ H O 0 A-3099 H H H H H CHF₂ C(═S)OCH₃ H O 0 A-3100 H H H H H CH₂CF₃ C(═S)OCH₃ H O 0 A-3101 H H H H H CH₂CHF₂ C(═S)OCH₃ H O 0 A-3102 H H H H H CH₂CCIF₂ C(═S)OCH₃ H O 0 A-3103 H H H H H CH₂CBrF₂ C(═S)OCH₃ H O 0 A-3104 H H H H H CF₂CF₃ C(═S)OCH₃ H O 0 A-3105 H H H H H CF₂CHF₂ C(═S)OCH₃ H O 0 A-3106 H H H H H CH₂CH₂CF₃ C(═S)OCH₃ H O 0

TABLE 52 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3107 H H H H H CH₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3108 H H H H H CH₂CF₂CHF₂ C(═S)OCH₃ H O 0 A-3109 H H H H H CF₂CHFCF₃ C(═S)OCH₃ H O 0 A-3110 H H H H H CF₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3111 H H H H H CH₂CF₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3112 H H H H H CH₂CF₂CHFCF₃ C(═S)OCH₃ H O 0 A-3113 H H H H H CH₂CH₂CH₂CF₃ C(═S)OCH₃ H O 0 A-3114 H H H H H CH₂CH₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3115 H H H H H CF₂CF₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3116 H H H H H CH₂CH₂CH(CF₃)₂ C(═S)OCH₃ H O 0 A-3117 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3118 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═S)OCH₃ H O 0 A-3119 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═S)OCH₃ H O 0 A-3120 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═S)OCH₃ H O 0 A-3121 H H H H H CH₂CH₂OCH₂CF₃ C(═S)OCH₃ H O 0 A-3122 H H H H H CF₂CHFOCF₃ C(═S)OCH₃ H O 0 A-3123 H H H H H CF₂CHFOCF₂CF₃ C(═S)OCH₃ H O 0 A-3124 H H H H H CH₂CH₂CF═CF₂ C(═S)OCH₃ H O 0 A-3125 H H H H H CH₂CH₂CH═CF₂ C(═S)OCH₃ H O 0 A-3126 H H H H H CH₂C≡CCH₃ C(═S)OCH₃ H O 0 A-3127 H H H H H CH₂C≡CCF₃ C(═S)OCH₃ H O 0 A-3128 H H H H H CH₂C≡CI C(═S)OCH₃ H O 0 A-3129 H H H H H CH₂(2,2-difluorocyclopropyl) C(═S)OCH₃ H O 0 A-3130 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═S)OCH₃ H O 0 A-3131 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═S)OCH₃ H O 0 A-3132 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═S)OCH₃ H O 0 A-3133 H H H H H CH₂SCH₃ C(═S)OCH₃ H O 0 A-3134 H H H H H CH₂SCH₂CH₃ C(═S)OCH₃ H O 0 A-3135 H H H H H CH₂CH₂SCH₃ C(═S)OCH₃ H O 0 A-3136 H H H H H CH₂SOCH₃ C(═S)OCH₃ H O 0 A-3137 H H H H H CH₂CH₂SOCH₃ C(═S)OCH₃ H O 0 A-3138 H H H H H CH₂SO₂CH₃ C(═S)OCH₃ H O 0 A-3139 H H H H H CH₂CH₂SO₂CH₃ C(═S)OCH₃ H O 0 A-3140 H H H H H CH₂SCF₃ C(═S)OCH₃ H O 0 A-3141 H H H H H CH₂SCHF₂ C(═S)OCH₃ H O 0 A-3142 H H H H H CH₂SCH₂CF₃ C(═S)OCH₃ H O 0 A-3143 H H H H H CH₂SCH₂CHF₂ C(═S)OCH₃ H O 0 A-3144 H H H H H CH₂SCF₂CF₃ C(═S)OCH₃ H O 0 A-3145 H H H H H CH₂CH₂SCF₃ C(═S)OCH₃ H O 0 A-3146 H H H H H CH₂SOCF₃ C(═S)OCH₃ H O 0 A-3147 H H H H H CH₂CH₂SOCF₃ C(═S)OCH₃ H O 0 A-3148 H H H H H CH₂CH₂CH₂SOCF₃ C(═S)OCH₃ H O 0 A-3149 H H H H H CH₂SO₂CF₃ C(═S)OCH₃ H O 0 A-3150 H H H H H CH₂CH₂SO₂CF₃ C(═S)OCH₃ H O 0 A-3151 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═S)OCH₃ H O 0 A-3152 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═S)OCH₃ H O 0 A-3153 H H H H H CH₂C(═O)NHCH₂CF₃ C(═S)OCH₃ H O 0 A-3154 H H H H H H C(═S)N(CH₃)₂ H O 0 A-3155 H H H H H CH₃ C(═S)N(CH₃)₂ H O 0 A-3156 H H H H H CH₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3157 H H H H H CH(CH₃)₂ C(═S)N(CH₃)₂ H O 0 A-3158 H H H H H CH₂CH₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3159 H H H H H CH₂CH(CH₃)₂ C(═S)N(CH₃)₂ H O 0 A-3160 H H H H H CH(CH₃)CH₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3161 H H H H H CH₂C(CH₃)₃ C(═S)N(CH₃)₂ H O 0 A-3162 H H H H H CH₂(CH₂)₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3163 H H H H H CH₂(CH₂)₃CH₃ C(═S)N(CH₃)₂ H O 0 A-3164 H H H H H CF₃ C(═S)N(CH₃)₂ H O 0 A-3165 H H H H H CHF₂ C(═S)N(CH₃)₂ H O 0 A-3166 H H H H H CH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3167 H H H H H CH₂CHF₂ C(═S)N(CH₃)₂ H O 0

TABLE 53 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3168 H H H H H CH₂CCIF₂ C(═S)N(CH₃)₂ H O 0 A-3169 H H H H H CH₂CBrF₂ C(═S)N(CH₃)₂ H O 0 A-3170 H H H H H CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3171 H H H H H CF₂CHF₂ C(═S)N(CH₃)₂ H O 0 A-3172 H H H H H CH₂CH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3173 H H H H H CH₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3174 H H H H H CH₂CF₂CHF₂ C(═S)N(CH₃)₂ H O 0 A-3175 H H H H H CF₂CHFCF₃ C(═S)N(CH₃)₂ H O 0 A-3176 H H H H H CF₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3177 H H H H H CH₂CF₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3178 H H H H H CH₂CF₂CHFCF₃ C(═S)N(CH₃)₂ H O 0 A-3179 H H H H H CH₂CH₂CH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3180 H H H H H CH₂CH₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3181 H H H H H CF₂CF₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3182 H H H H H CH₂CH₂CH(CF₃)₂ C(═S)N(CH₃)₂ H O 0 A-3183 H H H H H CF₂CF₂CF₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3184 H H H H H CH₂CF₂CF₂CF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3185 H H H H H CH₂CH₂CH₂CH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3186 H H H H H CH₂CF₂CF₂CF₂CHF₂ C(═S)N(CH₃)₂ H O 0 A-3187 H H H H H CH₂CH₂OCH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3188 H H H H H CF₂CHFOCF₃ C(═S)N(CH₃)₂ H O 0 A-3189 H H H H H CF₂CHFOCF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3190 H H H H H CH₂CH₂CF═CF₂ C(═S)N(CH₃)₂ H O 0 A-3191 H H H H H CH₂CH₂CH═CF₂ C(═S)N(CH₃)₂ H O 0 A-3192 H H H H H CH₂C≡CCH₃ C(═S)N(CH₃)₂ H O 0 A-3193 H H H H H CH₂C≡CCF₃ C(═S)N(CH₃)₂ H O 0 A-3194 H H H H H CH₂C≡CI C(═S)N(CH₃)₂ H O 0 A-3195 H H H H H CH₂(2,2-difluorocyclopropyl) C(═S)N(CH₃)₂ H O 0 A-3196 H H H H H CH₂(2,2-dichlorocyclopropyl) C(═S)N(CH₃)₂ H O 0 A-3197 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) C(═S)N(CH₃)₂ H O 0 A-3198 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) C(═S)N(CH₃)₂ H O 0 A-3199 H H H H H CH₂SCH₃ C(═S)N(CH₃)₂ H O 0 A-3200 H H H H H CH₂SCH₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3201 H H H H H CH₂CH₂SCH₃ C(═S)N(CH₃)₂ H O 0 A-3202 H H H H H CH₂SOCH₃ C(═S)N(CH₃)₂ H O 0 A-3203 H H H H H CH₂CH₂SOCH₃ C(═S)N(CH₃)₂ H O 0 A-3204 H H H H H CH₂SO₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3205 H H H H H CH₂CH₂SO₂CH₃ C(═S)N(CH₃)₂ H O 0 A-3206 H H H H H CH₂SCF₃ C(═S)N(CH₃)₂ H O 0 A-3207 H H H H H CH₂SCHF₂ C(═S)N(CH₃)₂ H O 0 A-3208 H H H H H CH₂SCH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3209 H H H H H CH₂SCH₂CHF₂ C(═S)N(CH₃)₂ H O 0 A-3210 H H H H H CH₂SCF₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3211 H H H H H CH₂CH₂SCF₃ C(═S)N(CH₃)₂ H O 0 A-3212 H H H H H CH₂SOCF₃ C(═S)N(CH₃)₂ H O 0 A-3213 H H H H H CH₂CH₂SOCF₃ C(═S)N(CH₃)₂ H O 0 A-3214 H H H H H CH₂CH₂CH₂SOCF₃ C(═S)N(CH₃)₂ H O 0 A-3215 H H H H H CH₂SO₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3216 H H H H H CH₂CH₂SO₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3217 H H H H H CH₂CH₂CH₂SO₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3218 H H H H H CH₂C(═O)NHCH₂CHF₂ C(═S)N(CH₃)₂ H O 0 A-3219 H H H H H CH₂C(═O)NHCH₂CF₃ C(═S)N(CH₃)₂ H O 0 A-3220 H H H H H H S(═O)₂CH₃ H O 0 A-3221 H H H H H CH₃ S(═O)₂CH₃ H O 0 A-3222 H H H H H CH₂CH₃ S(═O)₂CH₃ H O 0 A-3223 H H H H H CH(CH₃)₂ S(═O)₂CH₃ H O 0 A-3224 H H H H H CH₂CH₂CH₃ S(═O)₂CH₃ H O 0 A-3225 H H H H H CH₂CH(CH₃)₂ S(═O)₂CH₃ H O 0 A-3226 H H H H H CH(CH₃)CH₂CH₃ S(═O)₂CH₃ H O 0 A-3227 H H H H H CH₂C(CH₃)₃ S(═O)₂CH₃ H O 0 A-3228 H H H H H CH₂(CH₂)₂CH₃ S(═O)₂CH₃ H O 0

TABLE 54 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3229 H H H H H CH₂(CH₂)₃CH₃ S(═O)₂CH₃ H O 0 A-3230 H H H H H CF₃ S(═O)₂CH₃ H O 0 A-3231 H H H H H CHF₂ S(═O)₂CH₃ H O 0 A-3232 H H H H H CH₂CF₃ S(═O)₂CH₃ H O 0 A-3233 H H H H H CH₂CHF₂ S(═O)₂CH₃ H O 0 A-3234 H H H H H CH₂CCIF₂ S(═O)₂CH₃ H O 0 A-3235 H H H H H CH₂CBrF₂ S(═O)₂CH₃ H O 0 A-3236 H H H H H CF₂CF₃ S(═O)₂CH₃ H O 0 A-3237 H H H H H CF₂CHF₂ S(═O)₂CH₃ H O 0 A-3238 H H H H H CH₂CH₂CF₃ S(═O)₂CH₃ H O 0 A-3239 H H H H H CH₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3240 H H H H H CH₂CF₂CHF₂ S(═O)₂CH₃ H O 0 A-3241 H H H H H CF₂CHFCF₃ S(═O)₂CH₃ H O 0 A-3242 H H H H H CF₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3243 H H H H H CH₂CF₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3244 H H H H H CH₂CF₂CHFCF₃ S(═O)₂CH₃ H O 0 A-3245 H H H H H CH₂CH₂CH₂CF₃ S(═O)₂CH₃ H O 0 A-3246 H H H H H CH₂CH₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3247 H H H H H CF₂CF₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3248 H H H H H CH₂CH₂CH(CF₃)₂ S(═O)₂CH₃ H O 0 A-3249 H H H H H CF₂CF₂CF₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3250 H H H H H CH₂CF₂CF₂CF₂CF₃ S(═O)₂CH₃ H O 0 A-3251 H H H H H CH₂CH₂CH₂CH₂CF₃ S(═O)₂CH₃ H O 0 A-3252 H H H H H CH₂CF₂CF₂CF₂CHF₂ S(═O)₂CH₃ H O 0 A-3253 H H H H H CH₂CH₂OCH₂CF₃ S(═O)₂CH₃ H O 0 A-3254 H H H H H CF₂CHFOCF₃ S(═O)₂CH₃ H O 0 A-3255 H H H H H CF₂CHFOCF₂CF₃ S(═O)₂CH₃ H O 0 A-3256 H H H H H CH₂CH₂CF═CF₂ S(═O)₂CH₃ H O 0 A-3257 H H H H H CH₂CH₂CH═CF₂ S(═O)₂CH₃ H O 0 A-3258 H H H H H CH₂C≡CCH₃ S(═O)₂CH₃ H O 0 A-3259 H H H H H CH₂C≡CCF₃ S(═O)₂CH₃ H O 0 A-3260 H H H H H CH₂C≡CI S(═O)₂CH₃ H O 0 A-3261 H H H H H CH₂(2,2-difluorocyclopropyl) S(═O)₂CH₃ H O 0 A-3262 H H H H H CH₂(2,2-dichlorocyclopropyl) S(═O)₂CH₃ H O 0 A-3263 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) S(═O)₂CH₃ H O 0 A-3264 H H H H H CH₂CH₂(2,2-d)chlorocyclopropyl) S(═O)₂CH₃ H O 0 A-3265 H H H H H CH₂SCH₃ S(═O)₂CH₃ H O 0 A-3266 H H H H H CH₂SCH₂CH₃ S(═O)₂CH₃ H O 0 A-3267 H H H H H CH₂CH₂SCH₃ S(═O)₂CH₃ H O 0 A-3268 H H H H H CH₂SOCH₃ S(═O)₂CH₃ H O 0 A-3269 H H H H H CH₂CH₂SOCH₃ S(═O)₂CH₃ H O 0 A-3270 H H H H H CH₂SO₂CH₃ S(═O)₂CH₃ H O 0 A-3271 H H H H H CH₂CH₂SO₂CH₃ S(═O)₂CH₃ H O 0 A-3272 H H H H H CH₂SCF₃ S(═O)₂CH₃ H O 0 A-3273 H H H H H CH₂SCHF₂ S(═O)₂CH₃ H O 0 A-3274 H H H H H CH₂SCH₂CF₃ S(═O)₂CH₃ H O 0 A-3275 H H H H H CH₂SCH₂CHF₂ S(═O)₂CH₃ H O 0 A-3276 H H H H H CH₂SCF₂CF₃ S(═O)₂CH₃ H O 0 A-3277 H H H H H CH₂CH₂SCF₃ S(═O)₂CH₃ H O 0 A-3278 H H H H H CH₂SOCF₃ S(═O)₂CH₃ H O 0 A-3279 H H H H H CH₂CH₂SOCF₃ S(═O)₂CH₃ H O 0 A-3280 H H H H H CH₂CH₂CH₂SOCF₃ S(═O)₂CH₃ H O 0 A-3281 H H H H H CH₂SO₂CF₃ S(═O)₂CH₃ H O 0 A-3282 H H H H H CH₂CH₂SO₂CF₃ S(═O)₂CH₃ H O 0 A-3283 H H H H H CH₂CH₂CH₂SO₂CF₃ S(═O)₂CH₃ H O 0 A-3284 H H H H H CH₂C(═O)NHCH₂CHF₂ S(═O)₂CH₃ H O 0 A-3285 H H H H H CH₂C(═O)NHCH₂CF₃ S(═O)₂CH₃ H O 0 A-3286 H H H H H H S(═O)₂N(CH₃)₂ H O 0 A-3287 H H H H H CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3288 H H H H H CH₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3289 H H H H H CH(CH₃)₂ S(═O)₂N(CH₃)₂ H O 0

TABLE 55 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3290 H H H H H CH₂CH₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3291 H H H H H CH₂CH(CH₃)₂ S(═O)₂N(CH₃)₂ H O 0 A-3292 H H H H H CH(CH₃)CH₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3293 H H H H H CH₂C(CH₃)₃ S(═O)₂N(CH₃)₂ H O 0 A-3294 H H H H H CH₂(CH₂)₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3295 H H H H H CH₂(CH₂)₃CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3296 H H H H H CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3297 H H H H H CHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3298 H H H H H CH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3299 H H H H H CH₂CHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3300 H H H H H CH₂CCIF₂ S(═O)₂N(CH₃)₂ H O 0 A-3301 H H H H H CH₂CBrF₂ S(═O)₂N(CH₃)₂ H O 0 A-3302 H H H H H CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3303 H H H H H CF₂CHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3304 H H H H H CH₂CH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3305 H H H H H CH₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3306 H H H H H CH₂CF₂CHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3307 H H H H H CF₂CHFCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3308 H H H H H CF₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3309 H H H H H CH₂CF₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3310 H H H H H CH₂CF₂CHFCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3311 H H H H H CH₂CH₂CH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3312 H H H H H CH₂CH₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3313 H H H H H CF₂CF₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3314 H H H H H CH₂CH₂CH(CF₃)₂ S(═O)₂N(CH₃)₂ H O 0 A-3315 H H H H H CF₂CF₂CF₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3316 H H H H H CH₂CF₂CF₂CF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3317 H H H H H CH₂CH₂CH₂CH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3318 H H H H H CH₂CF₂CF₂CF₂CHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3319 H H H H H CH₂CH₂OCH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3320 H H H H H CF₂CHFOCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3321 H H H H H CF₂CHFOCF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3322 H H H H H CH₂CH₂CF═CF₂ S(═O)₂N(CH₃)₂ H O 0 A-3323 H H H H H CH₂CH₂CH═CF₂ S(═O)₂N(CH₃)₂ H O 0 A-3324 H H H H H CH₂C≡CCH₃ S(═O)₂N(CH₃)₂ H O 0 A-3325 H H H H H CH₂C≡CCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3326 H H H H H CH₂C≡CI S(═O)₂N(CH₃)₂ H O 0 A-3327 H H H H H CH₂(2,2- S(═O)₂N(CH₃)₂ H O 0 difluorocyclopropyl) A-3328 H H H H H CH₂(2,2- S(═O)₂N(CH₃)₂ H O 0 dichlorocyclopropyl) A-3329 H H H H H CH₂CH₂(2,2- S(═O)₂N(CH₃)₂ H O 0 difluorocyclopropyl) A-3330 H H H H H CH₂CH₂(2,2- S(═O)₂N(CH₃)₂ H O 0 dichlorocyclopropyl) A-3331 H H H H H CH₂SCH₃ S(═O)₂N(CH₃)₂ H O 0 A-3332 H H H H H CH₂SCH₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3333 H H H H H CH₂CH₂SCH₃ S(═O)₂N(CH₃)₂ H O 0 A-3334 H H H H H CH₂SOCH₃ S(═O)₂N(CH₃)₂ H O 0 A-3335 H H H H H CH₂CH₂SOCH₃ S(═O)₂N(CH₃)₂ H O 0 A-3336 H H H H H CH₂SO₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3337 H H H H H CH₂CH₂SO₂CH₃ S(═O)₂N(CH₃)₂ H O 0 A-3338 H H H H H CH₂SCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3339 H H H H H CH₂SCHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3340 H H H H H CH₂SCH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3341 H H H H H CH₂SCH₂CHF₂ S(═O)₂N(CH₃)₂ H O 0 A-3342 H H H H H CH₂SCF₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3343 H H H H H CH₂CH₂SCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3344 H H H H H CH₂SOCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3345 H H H H H CH₂CH₂SOCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3346 H H H H H CH₂CH₂CH₂SOCF₃ S(═O)₂N(CH₃)₂ H O 0 A-3347 H H H H H CH₂SO₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3348 H H H H H CH₂CH₂SO₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3349 H H H H H CH₂CH₂CH₂SO₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3350 H H H H H CH₂C(═O)NHCH₂CHF₂ S(═O)₂N(CH₃)₂ H O 0

TABLE 56 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3351 H H H H H CH₂C(═O)NHCH₂CF₃ S(═O)₂N(CH₃)₂ H O 0 A-3352 H H H H H H CH₂N(CH₃)₂ H O 0 A-3353 H H H H H CH₃ CH₂N(CH₃)₂ H O 0 A-3354 H H H H H CH₂CH₃ CH₂N(CH₃)₂ H O 0 A-3355 H H H H H CH(CH₃)₂ CH₂N(CH₃)₂ H O 0 A-3356 H H H H H CH₂CH₂CH₃ CH₂N(CH₃)₂ H O 0 A-3357 H H H H H CH₂CH(CH₃)₂ CH₂N(CH₃)₂ H O 0 A-3358 H H H H H CH(CH₃)CH₂CH₃ CH₂N(CH₃)₂ H O 0 A-3359 H H H H H CH₂C(CH₃)₃ CH₂N(CH₃)₂ H O 0 A-3360 H H H H H CH₂(CH₂)₃CH₃ CH₂N(CH₃)₂ H O 0 A-3361 H H H H H CH₂(CH₂)₂CH₃ CH₂N(CH₃)₂ H O 0 A-3362 H H H H H CF₃ CH₂N(CH₃)₂ H O 0 A-3363 H H H H H CHF₂ CH₂N(CH₃)₂ H O 0 A-3364 H H H H H CH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3365 H H H H H CH₂CHF₂ CH₂N(CH₃)₂ H O 0 A-3366 H H H H H CH₂CCIF₂ CH₂N(CH₃)₂ H O 0 A-3367 H H H H H CH₂CBrF₂ CH₂N(CH₃)₂ H O 0 A-3368 H H H H H CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3369 H H H H H CF₂CHF₂ CH₂N(CH₃)₂ H O 0 A-3370 H H H H H CH₂CH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3371 H H H H H CH₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3372 H H H H H CH₂CF₂CHF₂ CH₂N(CH₃)₂ H O 0 A-3373 H H H H H CF₂CHFCF₃ CH₂N(CH₃)₂ H O 0 A-3374 H H H H H CF₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3375 H H H H H CH₂CF₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3376 H H H H H CH₂CF₂CHFCF₃ CH₂N(CH₃)₂ H O 0 A-3377 H H H H H CH₂CH₂CH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3378 H H H H H CH₂CH₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3379 H H H H H CF₂CF₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3380 H H H H H CH₂CH₂CH(CF₃)₂ CH₂N(CH₃)₂ H O 0 A-3381 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3382 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3383 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3384 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂N(CH₃)₂ H O 0 A-3385 H H H H H CH₂CH₂OCH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3386 H H H H H CF₂CHFOCF₃ CH₂N(CH₃)₂ H O 0 A-3387 H H H H H CF₂CHFOCF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3388 H H H H H CH₂CH₂CF═CF₂ CH₂N(CH₃)₂ H O 0 A-3389 H H H H H CH₂CH₂CH═CF₂ CH₂N(CH₃)₂ H O 0 A-3390 H H H H H CH₂C≡CCH₃ CH₂N(CH₃)₂ H O 0 A-3391 H H H H H CH₂C≡CCF₃ CH₂N(CH₃)₂ H O 0 A-3392 H H H H H CH₂C≡CI CH₂N(CH₃)₂ H O 0 A-3393 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂N(CH₃)₂ H O 0 A-3394 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂N(CH₃)₂ H O 0 A-3395 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂N(CH₃)₂ H O 0 A-3396 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂N(CH₃)₂ H O 0 A-3397 H H H H H CH₂SCH₃ CH₂N(CH₃)₂ H O 0 A-3398 H H H H H CH₂SCH₂CH₃ CH₂N(CH₃)₂ H O 0 A-3399 H H H H H CH₂CH₂SCH₃ CH₂N(CH₃)₂ H O 0 A-3400 H H H H H CH₂SOCH₃ CH₂N(CH₃)₂ H O 0 A-3401 H H H H H CH₂CH₂SOCH₃ CH₂N(CH₃)₂ H O 0 A-3402 H H H H H CH₂SO₂CH₃ CH₂N(CH₃)₂ H O 0 A-3403 H H H H H CH₂CH₂SO₂CH₃ CH₂N(CH₃)₂ H O 0 A-3404 H H H H H CH₂SCF₃ CH₂N(CH₃)₂ H O 0 A-3405 H H H H H CH₂SCHF₂ CH₂N(CH₃)₂ H O 0 A-3406 H H H H H CH₂SCH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3407 H H H H H CH₂SCH₂CHF₂ CH₂N(CH₃)₂ H O 0 A-3408 H H H H H CH₂SCF₂CF₃ CH₂N(CH₃)₂ H O 0 A-3409 H H H H H CH₂CH₂SCF₃ CH₂N(CH₃)₂ H O 0 A-3410 H H H H H CH₂CH₂SOCF₃ CH₂N(CH₃)₂ H O 0 A-3411 H H H H H CH₂CH₂SOCF₃ CH₂N(CH₃)₂ H O 0

TABLE 57 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3412 H H H H H CH₂CH₂CH₂SOCF₃ CH₂N(CH₃)₂ H O 0 A-3413 H H H H H CH₂SO₂CF₃ CH₂N(CH₃)₂ H O 0 A-3414 H H H H H CH₂CH₂SO₂CF₃ CH₂N(CH₃)₂ H O 0 A-3415 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂N(CH₃)₂ H O 0 A-3416 H H H H H CH₂O(═O)NHCH₂CHF₂ CH₂N(CH₃)₂ H O 0 A-3417 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂N(CH₃)₂ H O 0 A-3418 H H H H H H CH₂(pyrrolidin-1-yl) H O 0 A-3419 H H H H H CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3420 H H H H H CH₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3421 H H H H H CH(CH₃)₂ CH₂(pyrrolidin-1-yl) H O 0 A-3422 H H H H H CH₂CH₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3423 H H H H H CH₂CH(CH₃)₂ CH₂(pyrrolidin-1-yl) H O 0 A-3424 H H H H H CH(CH₃)CH₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3425 H H H H H CH₂C(CH₃)₃ CH₂(pyrrolidin-1-yl) H O 0 A-3426 H H H H H CH₂(CH₂)₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3427 H H H H H CH₂(CH₂)₃CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3428 H H H H H CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3429 H H H H H CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3430 H H H H H CH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3431 H H H H H CH₂CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3432 H H H H H CH₂CCIF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3433 H H H H H CH₂CBrF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3434 H H H H H CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3435 H H H H H CF₂CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3436 H H H H H CH₂CH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3437 H H H H H CH₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3438 H H H H H CH₂CF₂CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3439 H H H H H CF₂CHFCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3440 H H H H H CF₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3441 H H H H H CH₂CF₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3442 H H H H H CH₂CF₂CHFCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3443 H H H H H CH₂CH₂CH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3444 H H H H H CH₂CH₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3445 H H H H H CF₂CF₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3446 H H H H H CH₂CH₂CH(CF₃)₂ CH₂(pyrrolidin-1-yl) H O 0 A-3447 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3448 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3449 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3450 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3451 H H H H H CH₂CH₂OCH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3452 H H H H H CF₂CHFOCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3453 H H H H H CF₂CHFOCF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3454 H H H H H CH₂CH₂CF═CF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3455 H H H H H CH₂CH₂CH═CF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3456 H H H H H CH₂C≡CCH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3457 H H H H H CH₂C≡CCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3458 H H H H H CH₂C≡CI CH₂(pyrrolidin-1-yl) H O 0 A-3459 H H H H H CH₂(2,2-dif1uorocyclopropyl) CH₂(pyrrolidin-1-yl) H O 0 A-3460 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂(pyrrolidin-1-yl) H O 0 A-3461 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂(pyrrolidin-1-yl) H O 0 A-3462 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂(pyrrolidin-1-yl) H O 0 A-3463 H H H H H CH₂SCH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3464 H H H H H CH₂SCH₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3465 H H H H H CH₂CH₂SCH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3466 H H H H H CH₂SOCH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3467 H H H H H CH₂CH₂SOCH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3468 H H H H H CH₂SO₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3469 H H H H H CH₂CH₂SO₂CH₃ CH₂(pyrrolidin-1-yl) H O 0 A-3470 H H H H H CH₂SCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3471 H H H H H CH₂SCHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3472 H H H H H CH₂SCH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0

TABLE 58 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3473 H H H H H CH₂SCH₂CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3474 H H H H H CH₂SCF₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3475 H H H H H CH₂CH₂SCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3476 H H H H H CH₂SOCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3477 H H H H H CH₂CH₂SOCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3478 H H H H H CH₂CH₂CH₂SOCF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3479 H H H H H CH₂SO₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3480 H H H H H CH₂CH₂SO₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3481 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3482 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂(pyrrolidin-1-yl) H O 0 A-3483 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂(pyrrolidin-1-yl) H O 0 A-3484 H H H H H H CH₂C(═O)OCH₃ H O 0 A-3485 H H H H H CH₃ CH₂C(═O)OCH₃ H O 0 A-3486 H H H H H CH₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3487 H H H H H CH(CH₃)₂ CH₂C(═O)OCH₃ H O 0 A-3488 H H H H H CH₂CH₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3489 H H H H H CH₂CH(CH₃)₂ CH₂C(═O)OCH₃ H O 0 A-3490 H H H H H CH(CH₃)CH₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3491 H H H H H CH₂C(CH₃)₃ CH₂C(═O)OCH₃ H O 0 A-3492 H H H H H CH₂(CH₂)₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3493 H H H H H CH₂(CH₂)₃CH₃ CH₂C(═O)OCH₃ H O 0 A-3494 H H H H H CF₃ CH₂C(═O)OCH₃ H O 0 A-3495 H H H H H CHF₂ CH₂C(═O)OCH₃ H O 0 A-3496 H H H H H CH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3497 H H H H H CH₂CHF₂ CH₂C(═O)OCH₃ H O 0 A-3498 H H H H H CH₂CCIF₂ CH₂C(═O)OCH₃ H O 0 A-3499 H H H H H CH₂CBrF₂ CH₂C(═O)OCH₃ H O 0 A-3500 H H H H H CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3501 H H H H H CF₂CHF₂ CH₂C(═O)OCH₃ H O 0 A-3502 H H H H H CH₂CH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3503 H H H H H CH₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3504 H H H H H CH₂CF₂CHF₂ CH₂C(═O)OCH₃ H O 0 A-3505 H H H H H CF₂CHFCF₃ CH₂C(═O)OCH₃ H O 0 A-3506 H H H H H CF₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3507 H H H H H CH₂CF₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3508 H H H H H CH₂CF₂CHFCF₃ CH₂C(═O)OCH₃ H O 0 A-3509 H H H H H CH₂CH₂CH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3510 H H H H H CH₂CH₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3511 H H H H H CF₂CF₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3512 H H H H H CH₂CH₂CH(CF₃)₂ CH₂C(═O)OCH₃ H O 0 A-3513 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3514 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3515 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3516 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂C(═O)OCH₃ H O 0 A-3517 H H H H H CH₂CH₂OCH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3518 H H H H H CF₂CHFOCF₃ CH₂C(═O)OCH₃ H O 0 A-3519 H H H H H CF₂CHFOCF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3520 H H H H H CH₂CH₂CF═CF₂ CH₂C(═O)OCH₃ H O 0 A-3521 H H H H H CH₂CH₂CH═CF₂ CH₂C(═O)OCH₃ H O 0 A-3522 H H H H H CH₂C≡CCH₃ CH₂C(═O)OCH₃ H O 0 A-3523 H H H H H CH₂C≡CCF₃ CH₂C(═O)OCH₃ H O 0 A-3524 H H H H H CH₂C≡CI CH₂C(═O)OCH₃ H O 0 A-3525 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂C(═O)OCH₃ H O 0 A-3526 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂C(═O)OCH₃ H O 0 A-3527 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂C(═O)OCH₃ H O 0 A-3528 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂C(═O)OCH₃ H O 0 A-3529 H H H H H CH₂SCH₃ CH₂C(═O)OCH₃ H O 0 A-3530 H H H H H CH₂SCH₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3531 H H H H H CH₂CH₂SCH₃ CH₂C(═O)OCH₃ H O 0 A-3532 H H H H H CH₂SOCH₃ CH₂C(═O)OCH₃ H O 0 A-3533 H H H H H CH₂CH₂SOCH₃ CH₂C(═O)OCH₃ H O 0

TABLE 59 Compound R¹ R² R³ R³ R⁵ R⁶ R⁷ R⁸ X n A-3534 H H H H H CH₂SO₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3535 H H H H H CH₂CH₂SO₂CH₃ CH₂C(═O)OCH₃ H O 0 A-3536 H H H H H CH₂SCF₃ CH₂C(═O)OCH₃ H O 0 A-3537 H H H H H CH₂SCHF₂ CH₂C(═O)OCH₃ H O 0 A-3538 H H H H H CH₂SCH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3539 H H H H H CH₂SCH₂CHF₂ CH₂C(═O)OCH₃ H O 0 A-3540 H H H H H CH₂SCF₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3541 H H H H H CH₂CH₂SCF₃ CH₂C(═O)OCH₃ H O 0 A-3542 H H H H H CH₂SOCF₃ CH₂C(═O)OCH₃ H O 0 A-3543 H H H H H CH₂CH₂SOCF₃ CH₂C(═O)OCH₃ H O 0 A-3544 H H H H H CH₂CH₂CH₂SOCF₃ CH₂C(═O)OCH₃ H O 0 A-3545 H H H H H CH₂SO₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3546 H H H H H CH₂CH₂SO₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3547 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3548 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂C(═O)OCH₃ H O 0 A-3549 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂C(═O)OCH₃ H O 0 A-3550 H H H H H H CH₂C(═O)NH₂ H O 0 A-3551 H H H H H CH₃ CH₂C(═O)NH₂ H O 0 A-3552 H H H H H CH₂CH₃ CH₂C(═O)NH₂ H O 0 A-3553 H H H H H CH(CH₃)₂ CH₂C(═O)NH₂ H O 0 A-3554 H H H H H CH₂CH₂CH₃ CH₂C(═O)NH₂ H O 0 A-3555 H H H H H CH₂CH(CH₃)₂ CH₂C(═O)NH₂ H O 0 A-3556 H H H H H CH(CH₃)CH₂CH₃ CH₂C(═O)NH₂ H O 0 A-3557 H H H H H CH₂C(CH₃)₃ CH₂C(═O)NH₂ H O 0 A-3558 H H H H H CH₂(CH₂)₂CH₃ CH₂C(═O)NH₂ H O 0 A-3559 H H H H H CH₂(CH₂)₃CH₃ CH₂C(═O)NH₂ H O 0 A-3560 H H H H H CF₃ CH₂C(═O)NH₂ H O 0 A-3561 H H H H H CHF₂ CH₂C(═O)NH₂ H O 0 A-3562 H H H H H CH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3563 H H H H H CH₂CHF₂ CH₂C(═O)NH₂ H O 0 A-3564 H H H H H CH₂CClF₂ CH₂C(═O)NH₂ H O 0 A-3565 H H H H H CH₂CBrF₂ CH₂C(═O)NH₂ H O 0 A-3566 H H H H H CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3567 H H H H H CF₂CHF₂ CH₂C(═O)NH₂ H O 0 A-3S68 H H H H H CH₂CH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3569 H H H H H CH₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3570 H H H H H CH₂CF₂CHF₂ CH₂C(═O)NH₂ H O 0 A-3571 H H H H H CF₂CHFCF₃ CH₂C(═O)NH₂ H O 0 A-3572 H H H H H CF₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3573 H H H H H CH₂CF₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3574 H H H H H CH₂CF₂CHFCF₃ CH₂C(═O)NH₂ H O 0 A-3575 H H H H H CH₂CH₂CH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3576 H H H H H CH₂CH₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3577 H H H H H CF₂CF₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3578 H H H H H CH₂CH₂CH(CF₃)₂ CH₂C(═O)NH₂ H O 0 A-3579 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3580 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3581 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3582 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂C(═O)NH₂ H O 0 A-3583 H H H H H CH₂CH₂OCH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3584 H H H H H CF₂CHFOCF₃ CH₂C(═O)NH₂ H O 0 A-3585 H H H H H CF₂CHFOCF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3586 H H H H H CH₂CH₂CF═CF₂ CH₂C(═O)NH₂ H O 0 A-3587 H H H H H CH₂CH₂CH═CF₂ CH₂C(═O)NH₂ H O 0 A-3588 H H H H H CH₂C≡CCH₃ CH₂C(═O)NH₂ H O 0 A-3589 H H H H H CH₂C≡CCF₃ CH₂C(═O)NH₂ H O 0 A-3590 H H H H H CH₂C≡CI CH₂C(═O)NH₂ H O 0 A-3591 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂C(═O)NH₂ H O 0 A-3592 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂C(═O)NH₂ H O 0 A-3593 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂C(═O)NH₂ H O 0 A-3594 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂C(═O)NH₂ H O 0

TABLE 60 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3595 H H H H H CH₂SCH₃ CH₂C(═O)NH₂ H O 0 A-3596 H H H H H CH₂SCH₂CH₃ CH₂C(═O)NH₂ H O 0 A-3597 H H H H H CH₂CH₂sCH₃ CH₂C(═O)NH₂ H O 0 A-3598 H H H H H CH₂SOCH₃ CH₂C(═O)NH₂ H O 0 A-3599 H H H H H CH₂CH₂SOCH₃ CH₂C(═O)NH₂ H O 0 A-3600 H H H H H CH₂SO₂CH₃ CH₂C(═O)NH₂ H O 0 A-3601 H H H H H CH₂CH₂SO₂CH₃ CH₂C(═O)NH₂ H O 0 A-3602 H H H H H CH₂SCF₃ CH₂C(═O)NH₂ H O 0 A-3603 H H H H H CH₂SCHF₂ CH₂C(═O)NH₂ H O 0 A-3604 H H H H H CH₂SCH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3605 H H H H H CH₂SCH₂CHF₂ CH₂C(═O)NH₂ H O 0 A-3606 H H H H H CH₂SCF₂CF₃ CH₂C(═O)NH₂ H O 0 A-3607 H H H H H CH₂CH₂SCF₃ CH₂C(═O)NH₂ H O 0 A-3608 H H H H H CH₂SOCF₃ CH₂C(═O)NH₂ H O 0 A-3609 H H H H H CH₂CH₂SOCF₃ CH₂C(═O)NH₂ H O 0 A-3610 H H H H H CH₂CH₂CH₂SOCF₃ CH₂C(═O)NH₂ H O 0 A-3611 H H H H H CH₂SO₂CF₃ CH₂C(═O)NH₂ H O 0 A-3612 H H H H H CH₂CH₂SO₂CF₃ CH₂C(═O)NH₂ H O 0 A-3613 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂C(═O)NH₂ H O 0 A-3614 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂C(═O)NH₂ H O 0 A-3615 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂C(═O)NH₂ H O 0 A-3616 H H H H H H CH═NOCH₃ H O 0 A-3617 H H H H H CH₃ CH═NOCH₃ H O 0 A-3618 H H H H H CH₂CH₃ CH═NOCH₃ H O 0 A-3619 H H H H H CH(CH₃)₂ CH═NOCH₃ H O 0 A-3620 H H H H H CH₂CH₂CH₃ CH═NOCH₃ H O 0 A-3621 H H H H H CH₂CH(CH₃)₂ CH═NOCH₃ H O 0 A-3622 H H H H H CH(CH₃)CH₂CH₃ CH═NOCH₃ H O 0 A-3623 H H H H H CH₂C(CH₃)₃ CH═NOCH₃ H O 0 A-3624 H H H H H CH₂(CH₂)₂CH₃ CH═NOCH₃ H O 0 A-3625 H H H H H CH₂(CH₂)₃CH₃ CH═NOCH₃ H O 0 A-3626 H H H H H CF₃ CH═NOCH₃ H O 0 A-3627 H H H H H CHF₂ CH═NOCH₃ H O 0 A-3628 H H H H H CH₂CF₃ CH═NOCH₃ H O 0 A-3629 H H H H H CH₂CHF₂ CH═NOCH₃ H O 0 A-3630 H H H H H CH₂CClF₂ CH═NOCH₃ H O 0 A-3631 H H H H H CH₂CBrF₂ CH═NOCH₃ H O 0 A-3632 H H H H H CF₂CF₃ CH═NOCH₃ H O 0 A-3633 H H H H H CF₂CHF₂ CH═NOCH₃ H O 0 A-3634 H H H H H CH₂CH₂CF₃ CH═NOCH₃ H O 0 A-3635 H H H H H CH₂CF₂CF₃ CH═NOCH₃ H O 0 A-3636 H H H H H CH₂CF₂CHF₂ CH═NOCH₃ H O 0 A-3637 H H H H H CF₂CHFCF₃ CH═NOCH₃ H O 0 A-3638 H H H H H CF₂CF₂CF₃ CH═NOCH₃ H O 0 A-3639 H H H H H CH₂CF₂CF₂CF₃ CH═NOCH₃ H O 0 A-3640 H H H H H CH₂CF₂CHFCF₃ CH═NOCH₃ H O 0 A-3641 H H H H H CH₂CH₂CH₂CF₃ CH═NOCH₃ H O 0 A-3642 H H H H H CH₂CH₂CF₂CF₃ CH═NOCH₃ H O 0 A-3643 H H H H H CF₂CF₂CF₂CF₃ CH═NOCH₃ H O 0 A-3644 H H H H H CH₂CH₂CH(CF₃)₂ CH═NOCH₃ H O 0 A-3645 H H H H H CF₂CF₂CF₂CF₂CF₃ CH═NOCH₃ H O 0 A-3646 H H H H H CH₂CF₂CF₂CF₂CF₃ CH═NOCH₃ H O 0 A-3647 H H H H H CH₂CH₂CH₂CH₂CF₃ CH═NOCH₃ H O 0 A-3648 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH═NOCH₃ H O 0 A-3649 H H H H H CH₂CH₂OCH₂CF₃ CH═NOCH₃ H O 0 A-3650 H H H H H CF₂CHFOCF₃ CH═NOCH₃ H O 0 A-3651 H H H H H CF₂CHFOCF₂CF₃ CH═NOCH₃ H O 0 A-3652 H H H H H CH₂CH₂CF═CF₂ CH═NOCH₃ H O 0 A-3653 H H H H H CH₂CH₂CH═CF₂ CH═NOCH₃ H O 0 A-3654 H H H H H CH₂C≡CCH₃ CH═NOCH₃ H O 0 A-3655 H H H H H CH₂C≡CCF₃ CH═NOCH₃ H O 0

TABLE 61 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3656 H H H H H CH₂C≡CI CH═NOCH₃ H O 0 A-3657 H H H H H CH₂(2,2-difluorocyclopropyl) CH═NOCH₃ H O 0 A-3658 H H H H H CH₂(2,2-dichlorocyclopropyl) CH═NOCH₃ H O 0 A-3659 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH═NOCH₃ H O 0 A-3660 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH═NOCH₃ H O 0 A-3661 H H H H H CH₂SCH₃ CH═NOCH₃ H O 0 A-3662 H H H H H CH₂SCH₂CH₃ CH═NOCH₃ H O 0 A-3663 H H H H H CH₂CH₂SCH₃ CH═NOCH₃ H O 0 A-3664 H H H H H CH₂SOCH₃ CH═NOCH₃ H O 0 A-3665 H H H H H CH₂CH₂SOCH₃ CH═NOCH₃ H O 0 A-3666 H H H H H CH₂SO₂CH₃ CH═NOCH₃ H O 0 A-3667 H H H H H CH₂CH₂SO₂CH₃ CH═NOCH₃ H O 0 A-3668 H H H H H CH₂SCF₃ CH═NOCH₃ H O 0 A-3669 H H H H H CH₂SCHF₂ CH═NOCH₃ H O 0 A-3670 H H H H H CH₂SCH₂CF₃ CH═NOCH₃ H O 0 A-3671 H H H H H CH₂SCH₂CHF₂ CH═NOCH₃ H O 0 A-3672 H H H H H CH_(z)SCF₂CF₃ CH═NOCH₃ H O 0 A-3673 H H H H H CH₂CH₂SCF₃ CH═NOCH₃ H O 0 A-3674 H H H H H CH₂SOCF₃ CH═NOCH₃ H O 0 A-3675 H H H H H CH₂CH₂SOCF₃ CH═NOCH₃ H O 0 A-3676 H H H H H CH₂CH₂CH₂SOCF₃ CH═NOCH₃ H O 0 A-3677 H H H H H CH₂SO₂CF₃ CH═NOCH₃ H O 0 A-3678 H H H H H CH₂CH₂SO₂CF₃ CH═NOCH₃ H O 0 A-3679 H H H H H CH₂CH₂CH₂SO₂CF₃ CH═NOCH₃ H O 0 A-3680 H H H H H CH₂C(═O)NHCH₂CHF₂ CH═NOCH₃ H O 0 A-3681 H H H H H CH₂C(═O)NHCH₂CF₃ CH═NOCH₃ H O 0 A-3682 H H H H H H ═CHN(CH₃)₂ O 0 A-3683 H H H H H CH₃ ═CHN(CH₃)₂ O 0 A-3684 H H H H H CH₂CH₃ ═CHN(CH₃)₂ O 0 A-3685 H H H H H CH(CH₃)₂ ═CHN(CH₃)₂ O 0 A-3686 H H H H H CH₂CH₂CH₃ ═CHN(CH₃)₂ O 0 A-3687 H H H H H CH₂CH(CH₃)₂ ═CHN(CH₃)₂ O 0 A-3688 H H H H H CH(CH₃)CH₂CH₂ ═CHN(CH₃)₂ O 0 A-3689 H H H H H CH₂C(CH₃)₃ ═CHN(CH₃)₂ O 0 A-3690 H H H H H CH₂(CH₂)₂CH₃ ═CHN(CH₃)₂ O 0 A-3691 H H H H H CH₂(CH₂)₃CH₃ ═CHN(CH₃)₂ O 0 A-3692 H H H H H CF₃ ═CHN(CH₃)₂ O 0 A-3693 H H H H H CHF₂ ═CHN(CH₃)₂ O 0 A-3694 H H H H H CH₂CF₃ ═CHN(CH₃)₂ O 0 A-3695 H H H H H CH₂CHF₂ ═CHN(CH₃)₂ O 0 A-3696 H H H H H CH₂CClF₂ ═CHN(CH₃)₂ O 0 A-3697 H H H H H CH₂CBrF₂ ═CHN(CH₃)₂ O 0 A-3698 H H H H H CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3699 H H H H H CF₂CHF₂ ═CHN(CH₃)₂ O 0 A-3700 H H H H H CH₂CH₂CF₃ ═CHN(CH₃)₂ O 0 A-3701 H H H H H CH₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3702 H H H H H CH₂CF₂CHF₂ ═CHN(CH₃)₂ O 0 A-3703 H H H H H CF₂CHFCF₃ ═CHN(CH₃)₂ O 0 A-3704 H H H H H CF₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3705 H H H H H CH₂CF₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3706 H H H H H CH₂CF₂CHFCF₃ ═CHN(CH₃)₂ O 0 A-3707 H H H H H CH₂CH₂CH₂CF₃ ═CHN(CH₃)₂ O 0 A-3708 H H H H H CH₂CH₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3709 H H H H H CF₂CF₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3710 H H H H H CH₂CH₂CH(CF₃)₂ ═CHN(CH₃)₂ O 0 A-3711 H H H H H CF₂CF₂CF₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3712 H H H H H CH₂CF₂CF₂CF₂CF₃ ═CHN(CH₃)₂ O 0 A-3713 H H H H H CH₂CH₂CH₂CH₂CF₃ ═CHN(CH₃)₂ O 0 A-3714 H H H H H CH₂CF₂CF₂CF₃CHF₂ ═CHN(CH₃)₂ O 0 A-3715 H H H H H CH₂CH₂OCH₂CF₃ ═CHN(CH₃)₂ O 0 A-3716 H H H H H CF₂CHFOCF₃ ═CHN(CH₃)₂ O 0

TABLE 62 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3717 H H H H H CF₂CHFOCF₂CF₃ ═CHN(CH₃)₂ O 0 A-3718 H H H H H CH₂CH₂CF═CF₂ ═CHN(CH₃)₂ O 0 A-3719 H H H H H CH₂CH₂CH═CF₂ ═CHN(CH₃)₂ O 0 A-3720 H H H H H CH₂C≡CCH₃ ═CHN(CH₃)₂ O 0 A-3721 H H H H H CH₂C≡CCF₃ ═CHN(CH₃)₂ O 0 A-3722 H H H H H CH₂C≡CI ═CHN(CH₃)₂ O 0 A-3723 H H H H H CH₂(2,2-difluorocyclopropyl) ═CHN(CH₃)₂ O 0 A-3724 H H H H H CH₂(2,2-dichlorocyclopropyl) ═CHN(CH₃)₂ O 0 A-3725 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) ═CHN(CH₃)₂ O 0 A-3726 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) ═CHN(CH₃)₂ O 0 A-3727 H H H H H CH₂SCH₃ ═CHN(CH₃)₂ O 0 A-3728 H H H H H CH₂SCH₂CH₃ ═CHN(CH₃)₂ O 0 A-3729 H H H H H CH₂CH₂SCH₃ ═CHN(CH₃)₂ O 0 A-3730 H H H H H CH₂SOCH₃ ═CHN(CH₃)₂ O 0 A-3731 H H H H H CH₂CH₂SOCH₃ ═CHN(CH₃)₂ O 0 A-3732 H H H H H CH₂SO₂CH₃ ═CHN(CH₃)₂ O 0 A-3733 H H H H H CH₂CH₂SO₂CH₃ ═CHN(CH₃)₂ O 0 A-3734 H H H H H CH₂SCF₃ ═CHN(CH₃)₂ O 0 A-3735 H H H H H CH₂SCHF₂ ═CHN(CH₃)₂ O 0 A-3736 H H H H H CH₂SCH₂CF₃ ═CHN(CH₃)₂ O 0 A-3737 H H H H H CH₂SCH₂CHF₂ ═CHN(CH₃)₂ O 0 A-3738 H H H H H CH₂SCF₂CF₃ ═CHN(CH₃)₂ O 0 A-3739 H H H H H CH₂CH₂SCF₃ ═CHN(CH₃)₂ O 0 A-3740 H H H H H CH₂SOCF₃ ═CHN(CH₃)₂ O 0 A-3741 H H H H H CH₂CH₂SOCF₃ ═CHN(CH₃)₂ O 0 A-3742 H H H H H CH₂CH₂CH₂SOCF₃ ═CHN(CH₃)₂ O 0 A-3743 H H H H H CH₂SO₂CF₃ ═CHN(CH₃)₂ O 0 A-3744 H H H H H CH₂CH₂SO₂CF₃ ═CHN(CH₃)₂ O 0 A-3745 H H H H H CH₂CH₂CH₂SO₂CF₃ ═CHN(CH₃)₂ O 0 A-3746 H H H H H CH₂C(═O)NHCH₂CHF₂ ═CHN(CH₃)₂ O 0 A-3747 H H H H H CH₂C(═O)NHCH₂CF₃ ═CHN(CH₃)₂ O 0 A-3748 H H H H H H CH₃ CH₃ O 0 A-3749 H H H H H CH₃ CH₃ CH₃ O 0 A-3750 H H H H H CH₂CH₃ CH₃ CH₃ O 0 A-3751 H H H H H CH(CH₃)₂ CH₃ CH₃ O 0 A-3752 H H H H H CH₂CH₂CH₃ CH₃ CH₃ O 0 A-3753 H H H H H CH₂CH(CH₃)₂ CH₃ CH₃ O 0 A-3754 H H H H H CH(CH₃)CH₂CH₃ CH₃ CH₃ O 0 A-3755 H H H H H CH₂C(CH₃)₃ CH₃ CH₃ O 0 A-3756 H H H H H CH₂(CH₂)₂CH₃ CH₃ CH₃ O 0 A-3757 H H H H H CH₂(CH₂)₃CH₃ CH₃ CH₃ O 0 A-3758 H H H H H CH₂(CH₂)₄CH₃ CH₃ CH₃ O 0 A-3759 H H H H H CH₂(CH₂)₆CH₃ CH₃ CH₃ O 0 A-3760 H H H H H CH₂OCH₃ CH₃ CH₃ O 0 A-3761 H H H H H CH₂OCH₂CH₃ CH₃ CH₃ O 0 A-3762 H H H H H CH₂CH₂OCH₃ CH₃ CH₃ O 0 A-3763 H H H H H CH₂CH₂OCH₂CH₃ CH₃ CH₃ O 0 A-3764 H H H H H CF₃ CH₃ CH₃ O 0 A-3765 H H H H H CHF₂ CH₃ CH₃ O 0 A-3766 H H H H H CH₂CF₃ CH₃ CH₃ O 0 A-3767 H H H H H CH₂CHF₂ CH₃ CH₃ O 0 A-3768 H H H H H CH₂CClF₂ CH₃ CH₃ O 0 A-3769 H H H H H CH₂CBrF₂ CH₃ CH₃ O 0 A-377O H H H H H CF₂CF₃ CH₃ CH₃ O 0 A-3771 H H H H H CF₂CHF₂ CH₃ CH₃ O 0 A-3772 H H H H H CH₂CH₂CF₃ CH₃ CH₃ O 0 A-3773 H H H H H CH₂CF₂CF₃ CH₃ CH₃ O 0 A-3774 H H H H H CH₂CF₂CHF₂ CH₃ CH₃ O 0 A-3775 H H H H H CF₂CHFCF₃ CH₃ CH₃ O 0 A-3776 H H H H H CF₂CF₂CF₃ CH₃ CH₃ O 0 A-3777 H H H H H CH₂CF₂CF₂CF₂ CH₃ CH₃ O 0

TABLE 63 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3778 H H H H H CH₂CF₂CHFCF₃ CH₃ CH₃ O 0 A-3779 H H H H H CH₂CH₂CH₂CF₃ CH₃ CH₃ O 0 A-3780 H H H H H CH₂CH₂CF₂CF₃ CH₃ CH₃ O 0 A-3781 H H H H H CF₂CF₂CF₂CF₃ CH₃ CH₃ O 0 A-3782 H H H H H CH₂CH₂CH(CF₃)₂ CH₃ CH₃ O 0 A-3783 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₃ CH₃ O 0 A-3784 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₃ CH₃ O 0 A-3785 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₃ CH₃ O 0 A-3786 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₃ CH₃ O 0 A-3787 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₃ CH₃ O 0 A 3788 H H H H H CF₂CHFOCH₃ CH₃ CH₃ O 0 A-3789 H H H H H CF₂CHFOCH₂CH₃ CH₃ CH₃ O 0 A-3790 H H H H H CH₂CH₂OCH₂CF₃ CH₃ CH₃ O 0 A-3791 H H H H H CF₂CHFOCF₃ CH₃ CH₃ O 0 A-3792 H H H H H CF₂CHFOCF₂CF₃ CH₃ CH₃ O 0 A-3793 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₃ CH₃ O 0 A-3794 H H H H H CH₂CH═CH₂ CH₃ CH₃ O 0 A-3795 H H H H H CH₂CH═CHCl CH₃ CH₃ O 0 A-3796 H H H H H CH₂CH═CCl₂ CH₃ CH₃ O 0 A-3797 H H H H H CH₂CH₂CF═CF₂ CH₃ CH₃ O 0 A-3798 H H H H H CH₂CH₂CH═CF₂ CH₃ CH₃ O 0 A-3799 H H H H H CH₂C≡CH CH₃ CH₃ O 0 A-3800 H H H H H CH₂C≡CCH₃ CH₃ CH₃ O 0 A-3801 H H H H H CH₂C≡CCF₃ CH₃ CH₃ O 0 A-3802 H H H H H CH₂C≡CI CH₃ CH₃ O 0 A-3803 H H H H H cyclobutyl CH₃ CH₃ O 0 A-3804 H H H H H cyclopentyl CH₃ CH₃ O 0 A-3805 H H H H H cyclohexyl CH₃ CH₃ O 0 A-3806 H H H H H 4,4-difluorocyclohexyl CH₃ CH₃ O 0 A-3807 H H H H H CH₂(cyclopropyl) CH₃ CH₃ O 0 A-3808 H H H H H CH₂(cyclobutyl) CH₃ CH₃ O 0 A-3809 H H H H H CH₂(cyclopentyl) CH₃ CH₃ O 0 A-3810 H H H H H CH₂CH₂(cyclopropyl) CH₃ CH₃ O 0 A-3811 H H H H H CH₂(2,2-difluorocyclopropyl) CH₃ CH₃ O 0 A-3812 H H H H H CH₂(2,2-dichlcrocyclopropyl) CH₃ CH₃ O 0 A-3813 H H H H H CH₂(4,4-difluorocyclohexyl) CH₃ CH₃ O 0 A-3814 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₃ CH₃ O 0 A-3815 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₃ CH₃ O 0 A-3816 H H H H H CH₂SCH₃ CH₃ CH₃ O 0 A-3817 H H H H H CH₂SCH₂CH₃ CH₃ CH₃ O 0 A-3818 H H H H H CH₂CH₂SCH₃ CH₃ CH₃ O 0 A-3819 H H H H H CH₂CH₂SCH₂CH₃ CH₃ CH₃ O 0 A-3820 H H H H H CH₂CH₂CH₂SCH₃ CH₃ CH₃ O 0 A-3821 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₃ CH₃ O 0 A-3822 H H H H H CH(CH₃)SCH₃ CH₃ CH₃ O 0 A-3823 H H H H H CH(CH₃)SCH₂CH₃ CH₃ CH₃ O 0 A-3824 H H H H H CH₂CH(CH₃)SCH₃ CH₃ CH₃ O 0 A-3825 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₃ CH₃ O 0 A-3826 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₃ CH₃ O 0 A-3827 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₃ CH₃ O 0 A-3828 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₃ CH₃ O 0 A-3829 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₃ CH₃ O 0 A-3830 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₃ CH₃ O 0 A-3831 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₃ CH₃ O 0 A-3832 H H H H H CH₂SOCH₃ CH₃ CH₃ O 0 A-3833 H H H H H CH₂CH₂SOCH₃ CH₃ CH₃ O 0 A-3834 H H H H H CH₂CH₂CH₂SOCH₃ CH₃ CH₃ O 0 A-3835 H H H H H CH(CH₃)SOCH₃ CH₃ CH₃ O 0 A-3836 H H H H H CH₂CH(CH₃)SOCH₃ CH₃ CH₃ O 0 A-3837 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₃ CH₃ O 0 A-3838 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₃ CH₃ O 0

TABLE 64 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3839 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₃ CH₃ O 0 A-3840 H H H H H CH₂SO₂CH₃ CH₃ CH₃ O 0 A-3841 H H H H H CH₂CH₂SO₂CH₃ CH₃ CH₃ O 0 A-3842 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₃ CH₃ O 0 A-3843 H H H H H CH(CH₃)SO₂CH₃ CH₃ CH₃ O 0 A-3844 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₃ CH₃ O 0 A-3845 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₃ CH₃ O 0 A-3846 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₃ CH₃ O 0 A-3847 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₃ CH₃ O 0 A-3848 H H H H H CH₂SCF₃ CH₃ CH₃ O 0 A-3849 H H H H H CH₂SCHF₂ CH₃ CH₃ O 0 A-3850 H H H H H CH₂SCH₂CF₃ CH₃ CH₃ O 0 A-3851 H H H H H CH₂SCH₂CHF₂ CH₃ CH₃ O 0 A-3852 H H H H H CH₂SCF₂CF₃ CH₃ CH₃ O 0 A-3853 H H H H H CH₂CH₂SCF₃ CH₃ CH₃ O 0 A-3854 H H H H H CH₂CH₂SCH₂CF₃ CH₃ CH₃ O 0 A-3855 H H H H H CH₂CH₂CH₂SCF₃ CH₃ CH₃ O 0 A-3856 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₃ CH₃ O 0 A-3857 H H H H H CH(CH₃)SCF₃ CH₃ CH₃ O 0 A-3858 H H H H H CH(CH₃)SCH₂CF₃ CH₃ CH₃ O 0 A-3859 H H H H H CH₂CH(CH₃)SCF₃ CH₃ CH₃ O 0 A-3860 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₃ CH₃ O 0 A-3861 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₃ CH₃ O 0 A-3862 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₃ CH₃ O 0 A-3863 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₃ CH₃ O 0 A-3864 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₃ CH₃ O 0 A-3865 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₃ CH₃ O 0 A-3866 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₃ CH₃ O 0 A-3867 H H H H H CH₂SOCF₃ CH₃ CH₃ O 0 A-3868 H H H H H CH₂CH₂SOCF₃ CH₃ CH₃ O 0 A-3869 H H H H H CH₂CH₂CH₂SOCF₃ CH₃ CH₃ O 0 A-3870 H H H H H CH(CH₃)SOCF₃ CH₃ CH₃ O 0 A-3871 H H H H H CH₂CH(CH₃)SOCF₃ CH₃ CH₃ O 0 A-3872 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₃ CH₃ O 0 A-3873 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₃ CH₃ O 0 A-3874 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₃ CH₃ O 0 A-3875 H H H H H CH₂SO₂CF₃ CH₃ CH₃ O 0 A-3876 H H H H H CH₂CH₂SO₂CF₃ CH₃ CH₃ O 0 A-3877 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₃ CH₃ O 0 A-3878 H H H H H CH(CH₃)SO₂CF₃ CH₃ CH₃ O 0 A-3879 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₃ CH₃ O 0 A-3880 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₃ CH₃ O 0 A-3881 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₃ CH₃ O 0 A-3882 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₃ CH₃ O 0 A-3883 H H H H H CH₂C(═O)CH₃ CH₃ CH₃ O 0 A-3884 H H H H H CH₂C(═O)CH₂CH₃ CH₃ CH₃ O 0 A-3885 H H H H H CH₂C(═O)C(CH₃)₃ CH₃ CH₃ O 0 A-3886 H H H H H CH₂CH₂C(═O)CH₃ CH₃ CH₃ O 0 A-3887 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₃ CH₃ O 0 A-3888 H H H H H CH₂C(═O)CF₃ CH₃ CH₃ O 0 A-3889 H H H H H CH₂CH₂C(═O)CF₃ CH₃ CH₃ O 0 A-3890 H H H H H CH₂C(═O)OCH₃ CH₃ CH₃ O 0 A-3891 H H H H H CH₂C(═O)OCH₂CH₃ CH₃ CH₃ O 0 A-3892 H H H H H CH₂C(═O)OC(CH₃)₃ CH₃ CH₃ O 0 A-3893 H H H H H CH₂CH₂C(═O)OCH₃ CH₃ CH₃ O 0 A-3894 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₃ CH₃ O 0 A-3895 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₃ CH₃ O 0 A-3896 H H H H H CH₂C(═O)NH₂ CH₃ CH₃ O 0 A-3897 H H H H H CH₂CH₂C(═O)NH₂ CH₃ CH₃ O 0 A-3898 H H H H H CH₂C(═O)NHCH₃ CH₃ CH₃ O 0 A-3899 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₃ CH₃ O 0

TABLE 65 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3900 H H H H H CH₂CH₂C(═O)NHCH₃ CH₃ CH₃ O 0 A-3901 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₃ CH₃ O 0 A-3902 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₃ CH₃ O 0 A-3903 H H H H H CH₂C(═O)NHCH₂CF₃ CH₃ CH₃ O 0 A-3904 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₃ CH₃ O 0 A-3905 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₃ CH₃ O 0 A-3906 H H H H H CH₂C(═O)N(CH₃)₂ CH₃ CH₃ O 0 A-3907 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₃ CH₃ O 0 A-3908 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₃ CH₃ O 0 A-3909 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₃ CH₃ O 0 A-3910 H H H H H CH₂CH₂OH CH₃ CH₃ O 0 A-3911 H H H H H CH₂CH(OH)CH₃ CH₃ CH₃ O 0 A-3912 H H H H H CH₂CH₂CH₂OH CH₃ CH₃ O 0 A-3913 H H H H H CH₂CH(OH)CH₂CH₃ CH₃ CH₃ O 0 A-3914 H H H H H CH₂CH(OH)C(CH₃)₃ CH₃ CH₃ O 0 A-3915 H H H H H CH₂CH₂CH(OH)CH₃ CH₃ CH₃ O 0 A-3916 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₃ CH₃ O 0 A-3917 H H H H H CH₂C(═NOH)CH₃ CH₃ CH₃ O 0 A-3918 H H H H H CH₂C(═NOH)CH₂CH₃ CH₃ CH₃ O 0 A-3919 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₃ CH₃ O 0 A-3920 H H H H H CH₂C(═NOCH₃)CH₃ CH₃ CH₃ O 0 A-3921 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₃ CH₃ O 0 A-3922 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH CH₃ O 0 A-3923 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₃ CH₃ O 0 A-3924 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₃ CH₃ O 0 A-3925 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₃ CH₃ O 0 A-3926 H H H H H CH₂Ph CH₃ CH₃ O 0 A-3927 H H H H H CH₂(2-F)Ph CH₃ CH₃ O 0 A-3928 H H H H H CH₂(3-F)Ph CH₃ CH₃ O 0 A-3929 H H H H H CH₂(4-F)Ph CH₃ CH₃ O 0 A-3930 H H H H H CH₂(2-Cl)Ph CH₃ CH₃ O 0 A-3931 H H H H H CH₂(3-Cl)Ph CH₃ CH₃ O 0 A-3932 H H H H H CH₂(4-Cl)Ph CH₃ CH₃ O 0 A-3933 H H H H H CH₂(2-CF₃)Ph CH₃ CH₃ O 0 A-3934 H H H H H CH₂(3-CF₃)Ph CH₃ CH₃ O 0 A-3935 H H H H H CH₂(4-CF₃)Ph CH₃ CH₃ O 0 A-3936 H H H H H CH₂(naphthalen-1-yl) CH₃ CH₃ O 0 A-3937 H H H H H CH₂(naphthalen-2-yl) CH₃ CH₃ O 0 A-3938 H H H H H CH₂CH₂Ph CH₃ CH₃ O 0 A-3939 H H H H H H CH₂CN CH₂CN O 0 A-3940 H H H H H CH₃ CH₂CN CH₂CN O 0 A-3941 H H H H H CH₂CH₃ CH₂CN CH₂CN O 0 A-3942 H H H H H CH(CH₃)₂ CH₂CN CH₂CN O 0 A-3943 H H H H H CH₂CH₂CH₃ CH₂CN CH₂CN O 0 A-3944 H H H H H CH₂CH(CH₃)₂ CH₂CN CH₂CN O 0 A-3945 H H H H H CH(CH₃)CH₂CH₃ CH₂CN CH₂CN O 0 A-3946 H H H H H CH₂C(CH₃)₃ CH₂CN CH₂CN O 0 A-3947 H H H H H CH₂(CH₂)₂CH₃ CH₃CN CH₂CN O 0 A-3948 H H H H H CH₂(CH₂)₃CH₃ CH₂CN CH₂CN O 0 A-3949 H H H H H CF₃ CH₂CN CH₂CN O 0 A-3950 H H H H H CHF₂ CH₂CN CH₂CN O 0 A-3951 H H H H H CH₂CF₃ CH₂CN CH₂CN O 0 A-3952 H H H H H CH₂CHF₂ CH₂CN CH₂CN O 0 A-3953 H H H H H CH₂CClF₂ CH₂CN CH₂CN O 0 A-3954 H H H H H CH₂CBrF₂ CH₂CN CH₂CN O 0 A-3955 H H H H H CF₂CF₃ CH₂CN CH₂CN O 0 A-3956 H H H H H CF₂CHF₂ CH₂CN CH₂CN O 0 A-3957 H H H H H CH₂CH₂CF₃ CH₂CN CH₂CN O 0 A-3958 H H H H H CH₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3959 H H H H H CH₂CF₂CHF₂ CH₂CN CH₂CN O 0 A-3960 H H H H H CF₂CHFCF₃ CH₂CN CH₂CN O 0

TABLE 66 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-3961 H H H H H CF₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3962 H H H H H CH₂CF₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3963 H H H H H CH₂CF₂CHFCF₃ CH₂CN CH₂CN O 0 A-3964 H H H H H CH₂CH₂CH₂CF₃ CH₂CN CH₂CN O 0 A-3965 H H H H H CH₂CH₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3966 H H H H H CF₂CF₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3967 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CN CH₂CN O 0 A-3968 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3969 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CN CH₂CN O 0 A-3970 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CN CH₂CN O 0 A-3971 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CN CH₂CN O 0 A-3972 H H H H H CH₂CH₂OCH₂CF₃ CH₂CN CH₂CN O 0 A-3973 H H H H H CF₂CHFOCF₃ CH₂CN CH₂CN O 0 A-3974 H H H H H CF₂CHFOCF₂CF₃ CH₂CN CH₂CN O 0 A-3975 H H H H H CH₂CH₂CF═CF₂ CH₂CN CH₂CN O 0 A-3976 H H H H H CH₂CH₂CH═CF₂ CH₂CN CH₂CN O 0 A-3977 H H H H H CH₂C≡CCH₃ CH₂CN CH₂CN O 0 A-3978 H H H H H CH₂C≡CCF₃ CH₂CN CH₂CN O 0 A-3979 H H H H H CH₂C≡CI CH₂CN CH₂CN O 0 A-3980 H H H H H CH₂(2,2-diflucrocyclopropyl) CH₂CN CH₂CN O 0 A-3981 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CN CH₂CN O 0 A-3982 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CN CH₂CN O 0 A-3983 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CN CH₂CN O 0 A-3984 H H H H H CH₂SCH₃ CH₂CN CH₂CN O 0 A-3985 H H H H H CH₂SCH₂CH₃ CH₂CN CH₂CN O 0 A-3986 H H H H H CH₂CH₂SCH₃ CH₂CN CH₂CN O 0 A-3987 H H H H H CH₂SOCH₃ CH₂CN CH₂CN O 0 A-3988 H H H H H CH₂CH₂SOCH₃ CH₂CN CH₂CN O 0 A-3989 H H H H H CH₂SO₂CH₃ CH₂CN CH₂CN O 0 A-3990 H H H H H CH₂CH₂SO₂CH₃ CH₂CN CH₂CN O 0 A-3991 H H H H H CH₂SCF₃ CH₂CN CH₂CN O 0 A-3992 H H H H H CH₂SCHF₂ CH₂CN CH₂CN O 0 A-3993 H H H H H CH₂SCH₂CF₃ CH₂CN CH₂CN O 0 A-3994 H H H H H CH₂SCH₂CHF₂ CH₂CN CH₂CN O 0 A-3995 H H H H H CH₂SCF₂CF₃ CH₂CN CH₂CN O 0 A-3996 H H H H H CH₂CH₂SCF₃ CH₂CN CH₂CN O 0 A-3997 H H H H H CH₂SOCF₃ CH₂CN CH₂CN O 0 A-3998 H H H H H CH₂CH₂SOCF₃ CH₂CN CH₂CN O 0 A-3999 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CN CH₂CN O 0 A-4000 H H H H H CH₂SO₂CF₃ CH₂CN CH₂CN O 0 A-4001 H H H H H CH₂CH₂SO₂CF₃ CH₂CN CH₂CN O 0 A-4002 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CN CH₂CN O 0 A-4003 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CN CH₂CN O 0 A-4004 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CN CH₂CN O 0 A-4005 H H H H H H —CH₂CH₂—O—CH₂CH₂— O 0 A-4006 H H H H H CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4007 H H H H H CH₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4008 H H H H H CH(CH₃)₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4009 H H H H H CH₂CH₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4010 H H H H H CH₂CH(CH₃)₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4011 H H H H H CH(CH₃)CH₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4012 H H H H H CH₂C(CH₃)₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4013 H H H H H CH₂(CH₂)₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4014 H H H H H CH₂(CH₂)₃CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4015 H H H H H CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4016 H H H H H CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4017 H H H H H CH₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4018 H H H H H CH₂CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4019 H H H H H CH₂CClF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4020 H H H H H CH₂CBrF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4021 H H H H H CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0

TABLE 67 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4022 H H H H H CF₃CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4023 H H H H H CH₂CH₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4024 H H H H H CH₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4025 H H H H H CH₂CF₂CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4026 H H H H H CF₂CHFCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4027 H H H H H CF₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4028 H H H H H CH₂CF₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4029 H H H H H CH₂CH₂CH₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4030 H H H H H CH₂CH₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4031 H H H H H CF₂CF₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4032 H H H H H CH₂CH₂CH(CF₃)₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4033 H H H H H CF₂CF₂CF₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4034 H H H H H CH₂CF₂CF₂CF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4035 H H H H H CH₂CH₂CH₂CH₃CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4036 H H H H H CH₂CF₂CF₂CF₂CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4037 H H H H H CH₂CH₂OCH₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4038 H H H H H CF₂CHFOCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4039 H H H H H CF₂CHFOCF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4040 H H H H H CH₂CH₂CF═CF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4041 H H H H H CH₂CH₂CH═CF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4042 H H H H H CH₂C≡CCH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4043 H H H H H CH₂C≡CCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4044 H H H H H CH₂C≡CI —CH₂CH₂—O—CH₂CH₂— O 0 A-4045 H H H H H CH₂(2,2-difluorocyclopropyl) —CH₂CH₂—O—CH₂CH₂— O 0 A-4046 H H H H H CH₂(2,2-dichlorocyclopropyl) —CH₂CH₂—O—CH₂CH₂— O 0 A-4047 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) —CH₂CH₂—O—CH₂CH₂— O 0 A-4048 H H H H H CH₂CH₂(2,2-diCHlorOcyclopropyl) —CH₂CH₂—O—CH₂CH₂— O 0 A-4049 H H H H H CH₂SCH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4050 H H H H H CH₂SCH₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4051 H H H H H CH₂CH₂SCH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4052 H H H H H CH₂SOCH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4053 H H H H H CH₂CH₂SOCH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4054 H H H H H CH₂SO₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4055 H H H H H CH₂CH₂SO₂CH₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4056 H H H H H CH₂SCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4057 H H H H H CH₂SCHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4058 H H H H H CH₂SCH₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4059 H H H H H CH₂SCH₂CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4060 H H H H H CH₂SCF₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4061 H H H H H CH₂CH₂SCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4062 H H H H H CH₂SOCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4063 H H H H H CH₂CH₂SOCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4064 H H H H H CH₂CH₂CH₂SOCF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4065 H H H H H CH₂SO₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4066 H H H H H CH₂CH₂SO₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4067 H H H H H CH₂CH₂CH₂SO₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4068 H H H H H CH₂C(═O)NHCH₂CHF₂ —CH₂CH₂—O—CH₂CH₂— O 0 A-4069 H H H H H CH₂C(═O)NHCH₂CF₃ —CH₂CH₂—O—CH₂CH₂— O 0 A-4070 H CF₃ H H H H H H O 0 A-4071 H CF₃ H H H CH₃ H H O 0 A-4072 H CF₃ H H H CH₂CH₃ H H O 0 A-4073 H CF₃ H H H CH(CH₃)₂ H H O 0 A-4074 H CF₃ H H H CH₂CH₂CH₃ H H O 0 A-4075 H CF₃ H H H CH₂CH(CH₃)₂ H H O 0 A-4076 H CF₃ H H H CH(CH₃)CH₂CH₃ H H O 0 A-4077 H CF₃ H H H CH₂C(CH₃)₃ H H O 0 A-4078 H CF₃ H H H CH₂(CH₂)₂CH₃ H H O 0 A-4079 H CF₃ H H H CH₂(CH₂)₃CH₃ H H O 0 A-4080 H CF₃ H H H CH₂(CH₂)₄CH₃ H H O 0 A-4081 H CF₃ H H H CH₂(CH₂)₆CH₃ H H O 0 A-4082 H CF₃ H H H CH₂OCH₃ H H O 0

TABLE 68 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4083 H CF₃ H H H CH₂OCH₂CH₃ H H O 0 A-4084 H CF₃ H H H CH₂CH₂OCH₃ H H O 0 A-4085 H CF₃ H H H CH₂CH₂OCH₂CH₃ H H O 0 A-4086 H CF₃ H H H CF₃ H H O 0 A-4087 H CF₃ H H H CHF₂ H H O 0 A-4088 H CF₃ H H H CH₂CF₃ H H O 0 A-4089 H CF₃ H H H CH₂CHF₂ H H O 0 A-4090 H CF₃ H H H CH₂CClF₂ H H O 0 A-4091 H CF₃ H H H CH₂CBrF₂ H H O 0 A-4092 H CF₃ H H H CF₂CF₃ H H O 0 A-4093 H CF₃ H H H CF₂CHF₂ H H O 0 A-4094 H CF₃ H H H CH₂CH₂CF₃ H H O 0 A-4095 H CF₃ H H H CH₂CF₂CF₃ H H O 0 A-4096 H CF₃ H H H CH₂CF₂CHF₂ H H O 0 A-4097 H CF₃ H H H CF₂CHFCF₃ H H O 0 A-4098 H CF₃ H H H CF₂CF₂CF₃ H H O 0 A-4099 H CF₃ H H H CH₂CF₂CF₂CF₃ H H O 0 A-4100 H CF₃ H H H CH₂CF₂CHFCF₃ H H O 0 A-4101 H CF₃ H H H CH₂CH₂CH₂CF₃ H H O 0 A-4102 H CF₃ H H H CH₂CH₂CF₂CF₃ H H O 0 A-4103 H CF₃ H H H CF₇CF₂CF₂CF₃ H H O 0 A-4104 H CF₃ H H H CH₂CH₂CH(CF₃)₂ H H O 0 A-4105 H CF₃ H H H CF₂CF₂CF₂CF₂CF₃ H H O 0 A-4106 H CF₃ H H H CH₂CF₂CF₂CF₂CF₃ H H O 0 A-4107 H CF₃ H H H CH₂CH₂CH₂CH₂CF₃ H H O 0 A-4108 H CF₃ H H H CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-4109 H CF₃ H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-4110 H CF₃ H H H CF₂CHFOCH₃ H H O 0 A-4111 H CF₃ H H H CF₂CHFOCH₂CH₃ H H O 0 A-4112 H CF₃ H H H CH₂CH₂OCH₂CF₃ H H O 0 A-4113 H CF₃ H H H CF₂CHFOCF₃ H H O 0 A-4114 H CF₃ H H H CF₂CHFOCF₂CF₃ H H O 0 A-4115 H CF₃ H H H CF₂CHFOCF₂CF₂CF₃ H H O 0 A-4116 H CF₃ H H H CH₂CH═CH₂ H H O 0 A-4117 H CF₃ H H H CH₂CH═CHCl H H O 0 A-4118 H CF₃ H H H CH₂CH═CCl₂ H H O 0 A-4119 H CF₃ H H H CH₂CH₂CF═CF₂ H H O 0 A-4120 H CF₃ H H H CH₂CH₂CH═CF₂ H H O 0 A-4121 H CF₃ H H H CH₂C≡CH H H O 0 A-4122 H CF₃ H H H CH₂C≡CCH₃ H H O 0 A-4123 H CF₃ H H H CH₂C≡CCF₃ H H O 0 A-4124 H CF₃ H H H CH₂C≡CI H H O 0 A-4125 H CF₃ H H H cyclobutyl H H O 0 A-4126 H CF₃ H H H cyclopentyl H H O 0 A-4127 H CF₃ H H H cyclohexyl H H O 0 A-4128 H CF₃ H H H 4,4-difluorocyclohexyl H H O 0 A-4129 H CF₃ H H H CH₂(cyclopropyl) H H O 0 A-4130 H CF₃ H H H CH₂(cyclobutyl) H H O 0 A-4131 H CF₃ H H H CH₂(cyclopentyl) H H O 0 A-4132 H CF₃ H H H CH₂CH₂(cyclopropyl) H H O 0 A-4133 H CF₃ H H H CH₂(2,2-difluorocyclopropyl) H H O 0 A-4134 H CF₃ H H H CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4135 H CF₃ H H H CH₂(4,4-difluorocyclohexyl) H H O 0 A-4136 H CF₃ H H H CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-4137 H CF₃ H H H CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4138 H CF₃ H H H CH₂SCH₃ H H O 0 A-4139 H CF₃ H H H CH₂SCH₂CH₃ H H O 0 A-4140 H CF₃ H H H CH₂CH₂SCH₃ H H O 0 A-4141 H CF₃ H H H CH₂CH₂SCH₂CH₃ H H O 0 A-4142 H CF₃ H H H CH₂CH₂CH₂SCH₃ H H O 0 A-4143 H CF₃ H H H CH₂CH₂CH₂SCH₂CH₃ H H O 0

TABLE 69 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4144 H CF₃ H H H CH(CH₃)SCH₃ H H O 0 A-4145 H CF₃ H H H CH(CH₃)SCH₂CH₃ H H O 0 A-4146 H CF₃ H H H CH₂CH(CH₃)SCH₃ H H O 0 A-4147 H CF₃ H H H CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4148 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-4149 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-4150 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-4151 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-4152 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-4153 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4154 H CF₃ H H H CH₂SOCH₃ H H O 0 A-4155 H CF₃ H H H CH₂CH₂SOCH₃ H H O 0 A-4156 H CF₃ H H H CH₂CH₂CH₂SOCH₃ H H O 0 A-4157 H CF₃ H H H CH(CH₃)SOCH₃ H H O 0 A-4158 H CF₃ H H H CH₂CH(CH₃)SOCH₃ H H O 0 A-4159 H CF₃ H H H CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-4160 H CF₃ H H H CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-4161 H CF₃ H H H CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-4162 H CF₃ H H H CH₂SO₂CH₃ H H O 0 A-4163 H CF₃ H H H CH₂CH₂SO₂CH₃ H H O 0 A-4164 H CF₃ H H H CH₂CH₂CH₂SC₂CH₃ H H O 0 A-4165 H CF₃ H H H CH(CH₃)SO₂CH₃ H H O 0 A-4166 H CF₃ H H H CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4167 H CF₃ H H H CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-4168 H CF₃ H H H CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-4169 H CF₃ H H H CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4170 H CF₃ H H H CH₂SCF₃ H H O 0 A-4171 H CF₃ H H H CH₂SCHF₂ H H O 0 A-4172 H CF₃ H H H CH₂SCH₂CF₃ H H O 0 A-4173 H CF₃ H H H CH₂SCH₂CHF₂ H H O 0 A-4174 H CF₃ H H H CH₂SCF₂CF₃ H H O 0 A-4175 H CF₃ H H H CH₂CH₂SCF₃ H H O 0 A-4176 H CF₃ H H H CH₂CH₂SCH₂CF₃ H H O 0 A-4177 H CF₃ H H H CH₂CH₂CH₂SCF₃ H H O 0 A-4178 H CF₃ H H H CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-4179 H CF₃ H H H CH(CH₃)SCF₃ H H O 0 A-4180 H CF₃ H H H CH(CH₃)SCH₂CF₃ H H O 0 A-4181 H CF₃ H H H CH₂CH(CH₃)SCF₃ H H O 0 A-4182 H CF₃ H H H CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4183 H CF₃ H H H CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-4184 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-4185 H CF₃ H H H CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-4186 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-4187 H CF₃ H H H CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-4188 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4189 H CF₃ H H H CH₂SOCF₃ H H O 0 A-4190 H CF₃ H H H CH₂CH₂SOCF₃ H H O 0 A-4191 H CF₃ H H H CH₂CH₂CH₂SOCF₃ H H O 0 A-4192 H CF₃ H H H CH(CH₃)SOCF₃ H H O 0 A-4193 H CF₃ H H H CH₂CH(CH₃)SOCF₃ H H O 0 A-4194 H CF₃ H H H CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-4195 H CF₃ H H H CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-4196 H CF₃ H H H CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-4197 H CF₃ H H H CH₂SO₂CF₃ H H O 0 A-4198 H CF₃ H H H CH₂CH₂SO₂CF₃ H H O 0 A-4199 H CF₃ H H H CH₂CH₂CH₂SO₂CF₃ H H O 0 A-4200 H CF₃ H H H CH(CH₃)SO₂CF₃ H H O 0 A-4201 H CF₃ H H H CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4202 H CF₃ H H H CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-4203 H CF₃ H H H CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-4204 H CF₃ H H H CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0

TABLE 70 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4205 H CF₃ H H H CH₂C(═O)CH₃ H H O 0 A-4206 H CF₃ H H H CH₂C(═O)CH₂CH₃ H H O 0 A-4207 H CF₃ H H H CH₂C(═O)C(CH₃)₃ H H O 0 A-4208 H CF₃ H H H CH₂CH₂C(═O)CH₃ H H O 0 A-4209 H CF₃ H H H CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-4210 H CF₃ H H H CH₂C(═O)CF₃ H H O 0 A-4211 H CF₃ H H H CH₂CH₂C(═O)CF₃ H H O 0 A-4212 H CF₃ H H H CH₂C(═O)OCH₃ H H O 0 A-4213 H CF₃ H H H CH₂C(═O)OCH₂CH₃ H H O 0 A-4214 H CF₃ H H H CH₂C(═O)OC(CH₃)₃ H H O 0 A-4215 H CF₃ H H H CH₂CH₂C(═O)OCH₃ H H O 0 A-4216 H CF₃ H H H CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-4217 H CF₃ H H H CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-4218 H CF₃ H H H CH₂C(═O)NH₂ H H O 0 A-4219 H CF₃ H H H CH₂CH₂C(═O)NH₂ H H O 0 A-4220 H CF₃ H H H CH₂C(═O)NHCH₃ H H O 0 A-4221 H CF₃ H H H CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4222 H CF₃ H H H CH₂CH₂C(═O)NHCH₃ H H O 0 A-4223 H CF₃ H H H CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4224 H CF₃ H H H CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4225 H CF₃ H H H CH₂C(═O)NHCH₂CF₃ H H O 0 A-4226 H CF₃ H H H CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4227 H CF₃ H H H CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-4228 H CF₃ H H H CH₂C(═O)N(CH₃)₂ H H O 0 A-4229 H CF₃ H H H CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4230 H CF₃ H H H CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-4231 H CF₃ H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4232 H CF₃ H H H CH₂CH₂OH H H O 0 A-4233 H CF₃ H H H CH₂CH(OH)CH₃ H H O 0 A-4234 H CF₃ H H H CH₂CH₂CH₂OH H H O 0 A-4235 H CF₃ H H H CH₂CH(OH)CH₂CH₃ H H O 0 A-4236 H CF₃ H H H CH₂CH(OH)C(CH₃)₃ H H O 0 A-4237 H CF₃ H H H CH₂CH₂CH(OH)CH₃ H H O 0 A-4238 H CF₃ H H H CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-4239 H CF₃ H H H CH₂C(═NOH)CH₃ H H O 0 A-4240 H CF₃ H H H CH₂C(═NOH)CH₂CH₃ H H O 0 A-4241 H CF₃ H H H CH₂C(═NOH)C(CH₃)₃ H H O 0 A-4242 H CF₃ H H H CH₂C(═NOCH₃)CH₃ H H O 0 A-4243 H CF₃ H H H CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-4244 H CF₃ H H H CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-4245 H CF₃ H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-4246 H CF₃ H H H CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-4247 H CF₃ H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-4248 H CF₃ H H H CH₂Ph H H O 0 A-4249 H CF₃ H H H CH₂(2-F)Ph H H O 0 A-4250 H CF₃ H H H CH₂(3-F)Ph H H O 0 A-4251 H CF₃ H H H CH₂(4-F)Ph H H O 0 A-4252 H CF₃ H H H CH₂(2-Cl)Ph H H O 0 A-4253 H CF₃ H H H CH₂(3-Cl)Ph H H O 0 A-4254 H CF₃ H H H CH₂(4-Cl)Ph H H O 0 A-4255 H CF₃ H H H CH₂(2-CF₃)Ph H H O 0 A-4256 H CF₃ H H H CH₂(3-CF₃)PH H H O 0 A-4257 H CF₃ H H H CH₂(4-CF₃)Ph H H O 0 A-4258 H CF₃ H H H CH₂(naphthalen-1-yl) H H O 0 A-4259 H CF₃ H H H CH₂(naphthalen-2-yl) H H O 0 A-4260 H CF₃ H H H CH₂CH₂Ph H H O 0 A-4261 H H F H H H H H O 0 A-4262 H H F H H CH₃ H H O 0 A-4263 H H F H H CH₂CH₃ H H O 0 A-4264 H H F H H CH(CH₃)₂ H H O 0 A-4265 H H F H H CH₂CH₂CH₃ H H O 0

TABLE 71 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4266 H H F H H CH₂CH(CH₃)₂ H H O 0 A-4267 H H F H H CH(CH₃)CH₂CH₃ H H O 0 A-4268 H H F H H CH₂C(CH₃)₃ H H O 0 A-4269 H H F H H CH_(?)(CH₂)₂CH₃ H H O 0 A-4270 H H F H H CH₂(CH₂)₃CH₃ H H O 0 A-4271 H H F H H CH₂(CH₂)₄CH₃ H H O 0 A-4272 H H F H H CH₂(CH₂)₆CH₃ H H O 0 A-4273 H H F H H CH₂OCH₃ H H O 0 A-4274 H H F H H CH₂OCH₂CH₃ H H O 0 A-4275 H H F H H CH₂CH₂OCH₃ H H O 0 A-4276 H H F H H CH₂CH₂OCH₂CH₃ H H O 0 A-4277 H H F H H CF₃ H H O 0 A-4278 H H F H H CHF₂ H H O 0 A-4279 H H F H H CH₂CF₃ H H O 0 A-4280 H H F H H CH₂CHF₂ H H O 0 A-4281 H H F H H CH₂CClF₂ H H O 0 A-4282 H H F H H CH₂CBrF₂ H H O 0 A-4283 H H F H H CF₂CF₃ H H O 0 A-4284 H H F H H CF₂CHF₂ H H O 0 A-4285 H H F H H CH₂CH₂CF₃ H H O 0 A-4286 H H F H H CH₂CF₂CF₃ H H O 0 A-4287 H H F H H CH₂CF₂CHF₂ H H O 0 A-4288 H H F H H CF₂CHFCF₃ H H O 0 A-4289 H H F H H CF₂CF₂CF₃ H H O 0 A-4290 H H F H H CH₂CF₂CF₂CF₃ H H O 0 A-4291 H H F H H CH2CF₂CHFCF₃ H H O 0 A-4292 H H F H H CH₂CH₂CH₂CF₃ H H O 0 A-4293 H H F H H CH₂CH₂CF₂CF₃ H H O 0 A-4294 H H F H H CF₂CF₂CF₂CF₃ H H O 0 A-4295 H H F H H CH₂CH₂CH(CF₃)₂ H H O 0 A-4296 H H F H H CF₂CF₂CF₂CF₂CF₃ H H O 0 A-4297 H H F H H CH₂CF₂CF₂CF₂CF₃ H H O 0 A-4298 H H F H H CH₂CH₂CH₂CH₂CF₃ H H O 0 A-4299 H H F H H CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-4300 H H F H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-4301 H H F H H CF₂CHFOCH₃ H H O 0 A-4302 H H F H H CF₂CHFOCH₂CH₃ H H O 0 A-4303 H H F H H CH₂CH₂OCH₂CF₃ H H O 0 A-4304 H H F H H CF₂CHFOCF₃ H H O 0 A-4305 H H F H H CF₂CHFOCF₂CF₃ H H O 0 A-4306 H H F H H CF₂CHFOCF₂CF₂CF₃ H H O 0 A-4307 H H F H H CH₂CH═CH₂ H H O 0 A-4308 H H F H H CH₂CH═CHCl H H O 0 A-4309 H H F H H CH₂CH═CCl₂ H H O 0 A-4310 H H F H H CH₂CH₂CF═CF₂ H H O 0 A-4311 H H F H H CH₂CH₂CH═CF₂ H H O 0 A-4312 H H F H H CH₂C≡CH H H O 0 A-4313 H H F H H CH₂C≡CCH₃ H H O 0 A-4314 H H F H H CH₂c≡CF₃ H H O 0 A-4315 H H F H H CH₂C≡CI H H O 0 A-4316 H H F H H cyclobutyl H H O 0 A-4317 H H F H H cyclopentyl H H O 0 A-4318 H H F H H cyclohexyl H H O 0 A-4319 H H F H H 4,4-difluorocyclohexyl H H O 0 A-4320 H H F H H CH₂(cyclopropyl) H H O 0 A-4321 H H F H H CH₂(cyclobutyl) H H O 0 A-4322 H H F H H CH₂(cyclopentyl) H H O 0 A-4323 H H F H H CH₂CH₂(cyclopropyl) H H O 0 A-4324 H H F H H CH₂(2,2-difluorocyclopropyl) H H O 0 A-4325 H H F H H CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4326 H H F H H CH₂(4,4-difluorocyclohexyl) H H O 0

TABLE 72 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4327 H H F H H CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-4328 H H F H H CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4329 H H F H H CH₂SCH₃ H H O 0 A-4330 H H F H H CH₂SCH₂CH₃ H H O 0 A-4331 H H F H H CH₂CH₂SCH₃ H H O 0 A-4332 H H F H H CH₂CH₂SCH₂CH₃ H H O 0 A-4333 H H F H H CH₂CH₂CH₂SCH₃ H H O 0 A-4334 H H F H H CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-4335 H H F H H CH(CH₃)SCH₃ H H O 0 A-4336 H H F H H CH(CH₃)SCH₂CH₃ H H O 0 A-4337 H H F H H CH₂CH(CH₃)SCH₃ H H O 0 A-4338 H H F H H CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4339 H H F H H CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-4340 H H F H H CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-4341 H H F H H CH₃CH(CH₃)CH₂SCH₃ H H O 0 A-4342 H H F H H CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-4343 H H F H H CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-4344 H H F H H CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4345 H H F H H CH₂SOCH₃ H H O 0 A-4346 H H F H H CH₂CH₂SOCH₃ H H O 0 A-4347 H H F H H CH₂CH₂CH₂SOCH₃ H H O 0 A-4348 H H F H H CH(CH₃)SOCH₃ H H O 0 A-4349 H H F H H CH₂CH(CH₃)SOCH₃ H H O 0 A-4350 H H F H H CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-4351 H H F H H CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-4352 H H F H H CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-4353 H H F H H CH₂SO₂CH₃ H H O 0 A-4354 H H F H H CH₂CH₂SO₂CH₃ H H O 0 A-4355 H H F H H CH₂CH₂CH₂SO₂CH₃ H H O 0 A-4356 H H F H H CH(CH₃)SO₂CH₃ H H O 0 A-4357 H H F H H CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4358 H H F H H CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-4359 H H F H H CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-4360 H H F H H CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4361 H H F H H CH₂SCF₃ H H O 0 A-4362 H H F H H CH₂SCHF₂ H H O 0 A-4363 H H F H H CH₂SCH₂CF₃ H H O 0 A-4364 H H F H H CH₂SCH₂CHF₂ H H O 0 A-4365 H H F H H CH₂SCF₂CF₃ H H O 0 A-4366 H H F H H CH₂CH₂SCF₃ H H O 0 A-4367 H H F H H CH₂CH₂SCH₂CF₃ H H O 0 A-4368 H H F H H CH₂CH₂CH₂SCF₃ H H O 0 A-4369 H H F H H CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-4370 H H F H H CH(CH₃)SCF₃ H H O 0 A-4371 H H F H H CH(CH₃)SCH₂CF₃ H H O 0 A-4372 H H F H H CH₂CH(CH₃)SCF₃ H H O 0 A-4373 H H F H H CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4374 H H F H H CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-4375 H H F H H CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-4376 H H F H H CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-4377 H H F H H CH₂CH(CH₃)CH₃SCH₂CF₃ H H O 0 A-4378 H H F H H CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-4379 H H F H H CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4380 H H F H H CH₂SOCF₃ H H O 0 A-4381 H H F H H CH₂CH₂SOCF₃ H H O 0 A-4382 H H F H H CH₂CH₂CH₂SOCF₃ H H O 0 A-4383 H H F H H CH(CH₃)SOCF₃ H H O 0 A-4384 H H F H H CH₂CH(CH₃)SOCF₂ H H O 0 A-4385 H H F H H CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-4386 H H F H H CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-4387 H H F H H CH₂CH₂CH(CH₃)SOCF₃ H H O 0

TABLE 73 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4388 H H F H H CH₂SO₂CF₃ H H O 0 A-4389 H H F H H CH₂CH₂SO₂CF₃ H H O 0 A-4390 H H F H H CH₂CH₂CH₂SO₂CF₃ H H O 0 A-4391 H H F H H CH(CH₃)SO₂CF₃ H H O 0 A-4392 H H F H H CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4393 H H F H H CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-4394 H H F H H CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-4395 H H F H H CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4396 H H F H H CH₂C(═O)CH₃ H H O 0 A-4397 H H F H H CH₂C(═O)CH,CH₃ H H O 0 A-4398 H H F H H CH₂C(═O)C(CH₃)₃ H H O 0 A-4399 H H F H H CH₂CH₂C(═O)CH₃ H H O 0 A-4400 H H F H H CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-4401 H H F H H CH₂C(═O)CF₃ H H O 0 A-4402 H H F H H CH₂CH₂C(═O)CF₃ H H O 0 A-4403 H H F H H CH₂C(═O)OCH₃ H H O 0 A-4404 H H F H H CH₂C(═O)OCH₂CH₃ H H O 0 A-4405 H H F H H CH₂C(═O)OC(CH₃)₃ H H O 0 A-4406 H H F H H CH₂CH₂C(═O)OCH₃ H H O 0 A-4407 H H F H H CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-4408 H H F H H CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-4409 H H F H H CH₂C(═O)NH₂ H H O 0 A-4410 H H F H H CH₂CH₂C(═O)NH₂ H H O 0 A-4411 H H F H H CH₂C(═O)NHCH₃ H H O 0 A-4412 H H F H H CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4413 H H F H H CH₂CH₂C(═O)NHCH₃ H H O 0 A-4414 H H F H H CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4415 H H F H H CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4416 H H F H H CH₂C(═O)NHCH₂CF₃ H H O 0 A-4417 H H F H H CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4418 H H F H H CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-4419 H H F H H CH₂C(═O)N(CH₃)₂ H H O 0 A-4420 H H F H H CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4421 H H F H H CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-4422 H H F H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4423 H H F H H CH₂CH₂OH H H O 0 A-4424 H H F H H CH₂CH(OH)CH₃ H H O 0 A-4425 H H F H H CH₂CH₂CH₂OH H H O 0 A-4426 H H F H H CH₂CH(OH)CH₂CH₃ H H O 0 A-4427 H H F H H CH₂CH(OH)C(CH₃)₃ H H O 0 A 4428 H H F H H CH₂CH₂CH(OH)CH₃ H H O 0 A-4429 H H F H H CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-4430 H H F H H CH₂C(═NOH)CH₃ H H O 0 A-4431 H H F H H CH₂C(═NOH)CH₂CH₃ H H O 0 A-4432 H H F H H CH₂C(═NOH)C(CH₃)₃ H H O 0 A-4433 H H F H H CH₂C(═NOCH₃)CH₃ H H O 0 A-4434 H H F H H CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-4435 H H F H H CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-4436 H H F H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-4437 H H F H H CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-4438 H H F H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-4439 H H F H H CH₂Ph H H O 0 A-4440 H H F H H CH₂(2-F)Ph H H O 0 A-4441 H H F H H CH₂(3-F)Ph H H O 0 A-4442 H H F H H CH₂(4-F)Ph H H O 0 A-4443 H H F H H CH₂(2-Cl)Ph H H O 0 A-4444 H H F H H CH₂(3-Cl)Ph H H O 0 A-4445 H H F H H CH₂(4-Cl)Ph H H O 0 A-4446 H H F H H CH₂(2-CF₃)Ph H H O 0 A-4447 H H F H H CH₂(3-CF₃)Ph H H O 0 A-4448 H H F H H CH₂(4-CF₃)Ph H H O 0

TABLE 74 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4449 H H H H H CH₂(naphthalen-1-yl) H H O 0 A-4450 H H H H H CH₂(naphthalen-2-yl) H H O 0 A-4451 H H H H H CH₂CH₂Ph H H O 0 A-4452 Cl H H H H H H H O 0 A-4453 Cl H H H H CH₃ H H O 0 A-4454 Cl H H H H CH₂CH₃ H H O 0 A-4455 Cl H H H H CH(CH₃)₂ H H O 0 A-4455 Cl H H H H CH₂CH₂CH₃ H H O 0 A-4457 Cl H H H H CH₂CH(CH₃)₂ H H O 0 A-4458 Cl H H H H CH(CH₃)CH₂CH₃ H H O 0 A-4459 Cl H H H H CH₂C(CH₃)₃ H H O 0 A-4460 Cl H H H H CH₂(CH₂)₂CH₃ H H O 0 A-4451 Cl H H H H CH₂(CH₂)₃CH₃ H H O 0 A-4462 Cl H H H H CH₂(CH₂)₄CH₃ H H O 0 A-4463 Cl H H H H CH₂(CH₂)₆CH₃ H H O 0 A-4464 Cl H H H H CH₂OCH₃ H H O 0 A-4465 Cl H H H H CH₂OCH₂CH₃ H H O 0 A-4466 Cl H H H H CH₂CH₂OCH₃ H H O 0 A-4467 Cl H H H H CH₂CH₂OCH₂CH₃ H H O 0 A-4458 Cl H H H H CF₃ H H O 0 A-4459 Cl H H H H CHF₂ H H O 0 A-4470 Cl H H H H CH₂CF₃ H H O 0 A-4471 Cl H H H H CH₂CHF₂ H H O 0 A-4472 Cl H H H H CH₂CClF₂ H H O 0 A-4473 Cl H H H H CH₂CBrF₂ H H O 0 A-4474 Cl H H H H CF₂CF₃ H H O 0 A-4475 Cl H H H H CF₂CHF₂ H H O 0 A-4476 Cl H H H H CH₂CH₂CF₃ H H O 0 A-4477 Cl H H H H CH₂CF₂CF₃ H H O 0 A-4478 Cl H H H H CH₂CF₂CHF₂ H H O 0 A-4479 Cl H H H H CF₂CHFCF₃ H H O 0 A-4480 Cl H H H H CF₂CF₂CF₃ H H O 0 A-4481 Cl H H H H CH₂CF₂CF₂CF₃ H H O 0 A-4482 Cl H H H H CH₂CH₂CH₂CF₃ H H O 0 A-4483 Cl H H H H CH₂CH₂CF₂CF₃ H H O 0 A-4484 Cl H H H H CF₂CF₂CF₂CF₃ H H O 0 A-4485 Cl H H H H CH₂CH₂CH(CF₃)₂ H H O 0 A-4486 Cl H H H H CF₂CF₂CF₂CF₂CF₃ H H O 0 A-4487 Cl H H H H CH₂CF₂CF₂CF₂CF₃ H H O 0 A-4488 Cl H H H H CH₂CH₂CH₂CH₂CF₃ H H O 0 A-4489 Cl H H H H CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-4490 Cl H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-4491 Cl H H H H CF₂CHFOCH₃ H H O 0 A-4492 Cl H H H H CF₂CHFOCH₂CH₃ H H O 0 A-4493 Cl H H H H CH₂CH₂OCH₂CF₃ H H O 0 A-4494 Cl H H H H CF₂CHFOCF₃ H H O 0 A-4495 Cl H H H H CF₂CHFOCF₂CF₃ H H O 0 A-4495 Cl H H H H CF₂CHFOCF₂CF₂CF₃ H H O 0 A-4497 Cl H H H H CH₂CH═CH₂ H H O 0 A-4498 Cl H H H H CH₂CH═CHCl H H O 0 A-4499 Cl H H H H CH₂CH═CCl₂ H H O 0 A-4500 Cl H H H H CH₂CH₂CF═CF₂ H H O 0 A-4501 Cl H H H H CH₂CH₂CH═CF₂ H H O 0 A-4502 Cl H H H H CH₂C≡CH H H O 0 A-4503 Cl H H H H CH₂C≡CCH₃ H H O 0 A-4504 Cl H H H H CH₂C≡CF₃ H H O 0 A-4505 Cl H H H H CH₂C≡Cl H H O 0 A-4506 Cl H H H H cyclobutyl H H O 0 A-4507 Cl H H H H cyclopentyl H H O 0 A-4508 Cl H H H H cyclohexyl H H O 0 A-4509 Cl H H H H 4,4-difluorocyclohexyl H H O 0

TABLE 75 Compound R¹ R² R³ R³ R^(S) R⁶ R⁷ R⁸ X n A-4510 Cl H H H H CH₂(cyclopropyl) H H O 0 A-4511 Cl H H H H CH₂(cyclobutyl) H H O 0 A-4512 Cl H H H H CH₂(cyclopertyl) H H O 0 A-4513 Cl H H H H CH₂CH₂(cyclopropyl) H H O 0 A-4514 Cl H H H H CH₂(2,2-difluorocyclopropyl) H H O 0 A-4515 Cl H H H H CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4516 Cl H H H H CH₂(4,4-difluorocyclohexyl) H H O 0 A-4517 Cl H H H H CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-4518 Cl H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4519 Cl H H H H CH₂SCH₃ H H O 0 A-4520 Cl H H H H CH₂SCH₂CH₃ H H O 0 A-4521 Cl H H H H CH₂CH₂SCH₃ H H O 0 A-4522 Cl H H H H CH₂CH₂SCH₂CH₃ H H O 0 A-4523 Cl H H H H CH₂CH₂CH₂SCH₃ H H O 0 A-4524 Cl H H H H CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-4525 Cl H H H H CH(CH₃)SCH₃ H H O 0 A-4526 Cl H H H H CH(CH₃)SCH₂CH₃ H H O 0 A-4527 Cl H H H H CH₂CH(CH₃)SCH₃ H H O 0 A-4528 Cl H H H H CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4529 Cl H H H H CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-4530 Cl H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-4531 Cl H H H H CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-4532 Cl H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-4533 Cl H H H H CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-4534 Cl H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4535 Cl H H H H CH₂SOCH₃ H H O 0 A-4536 Cl H H H H CH₂CH₂SOCH₃ H H O 0 A-4537 Cl H H H H CH₂CH₂CH₂SOCH₃ H H O 0 A-4538 Cl H H H H CH(CH₃)SOCH₃ H H O 0 A-4539 Cl H H H H CH₂CH(CH₃)SOCH₃ H H O 0 A-4540 Cl H H H H CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-4541 Cl H H H H CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-4542 Cl H H H H CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-4543 Cl H H H H CH₂SO₂CH₃ H H O 0 A-4544 Cl H H H H CH₂CH₂SO₂CH₃ H H O 0 A-4545 Cl H H H H CH₂CH₂CH₂SO₂CH₃ H H O 0 A-4546 Cl H H H H CH(CH₃)SO₂CH₃ H H O 0 A-4547 Cl H H H H CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4548 Cl H H H H CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-4549 Cl H H H H CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-4550 Cl H H H H CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4S51 Cl H H H H CH₂SCF₃ H H O 0 A-4552 Cl H H H H CH₂SCHF₂ H H O 0 A-4553 Cl H H H H CH₂SCH₂CF₃ H H O 0 A-4554 Cl H H H H CH₂SCH₂CHF₂ H H O 0 A-4555 Cl H H H H CH₂SCF₂CF₃ H H O 0 A-4556 Cl H H H H CH₂CH₂SCF₃ H H O 0 A-4557 Cl H H H H CH₂CH₂SCH₂CF₃ H H O 0 A-4558 Cl H H H H CH₂CH₂CH₂SCF₃ H H O 0 A-4559 Cl H H H H CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-4560 Cl H H H H CH(CH₃)SCF₃ H H O 0 A-4561 Cl H H H H CH(CH₃)SCH₂CF₃ H H O 0 A-4562 Cl H H H H CH₂CH(CH₃)SCF₃ H H O 0 A-4563 Cl H H H H CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4564 Cl H H H H CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-4565 Cl H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-4566 Cl H H H H CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-4567 Cl H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-4568 Cl H H H H CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-4569 Cl H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4570 Cl H H H H CH₂SOCF₃ H H O 0

TABLE 76 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4571 Cl H H H H CH₂CH₂SOCF₃ H H O 0 A 4572 Cl H H H H CH₂CH₂CH₂SOCF₃ H H O 0 A-4573 Cl H H H H CH(CH₃)SOCF₃ H H O 0 A-4574 Cl H H H H CH₂CH(CH₃)SOCF₃ H H O 0 A-4575 Cl H H H H CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-4576 Cl H H H H CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-4577 Cl H H H H CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-4578 Cl H H H H CH₂SO₂CF₃ H H O 0 A-4579 Cl H H H H CH₂CH₂SO₂CF₃ H H O 0 A-4580 Cl H H H H CH₂CH₂CH₂SO₂CF₃ H H O 0 A-4581 Cl H H H H CH(CH₃)SO₂CF₃ H H O 0 A-4582 Cl H H H H CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4583 Cl H H H H CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-4584 Cl H H H H CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-4585 Cl H H H H CH₂CH₂CH(CH₃₎SO₂CF₃ H H O 0 A-4586 Cl H H H H CH₂C(═O)CH₃ H H O 0 A-4587 Cl H H H H CH₂C(═O)CH₂CH₃ H H O 0 A-4588 Cl H H H H CH₂C(═O)C(CH₃)₃ H H O 0 A-4589 Cl H H H H CH₂CH₂C(═O)CH₃ H H O 0 A-4590 Cl H H H H CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-4591 Cl H H H H CH₂C(═O)CF₃ H H O 0 A-4592 Cl H H H H CH₂CH₂C(═O)CF₃ H H O 0 A-4593 Cl H H H H CH₂C(═O)OCH₃ H H O 0 A-4594 Cl H H H H CH₂C(═O)OCH₂CH₃ H H O 0 A-4595 Cl H H H H CH₂C(═O)OC(CH₃)₃ H H O 0 A-4596 Cl H H H H CH₂CH₂C(═O)OCH₃ H H O 0 A-4597 Cl H H H H CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-4598 Cl H H H H CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-4599 Cl H H H H CH₂C(═O)NH₂ H H O 0 A-4600 Cl H H H H CH₂CH₂C(═O)NH₂ H H O 0 A-4601 Cl H H H H CH₂C(═O)NHCH₃ H H O 0 A-4602 Cl H H H H CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4603 Cl H H H H CH₂CH₂C(═O)NHCH₃ H H O 0 A-4604 Cl H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4605 Cl H H H H CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4606 Cl H H H H CH₂C(═O)NHCH₂CF₃ H H O 0 A-4607 Cl H H H H CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4608 Cl H H H H CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-4609 Cl H H H H CH₂C(═O)N(CH₃)₂ H H O 0 A-4610 Cl H H H H CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4611 Cl H H H H CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-4612 Cl H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4613 Cl H H H H CH₂CH₂OH H H O 0 A-4614 Cl H H H H CH₂CH(OH)CH₃ H H O 0 A-4615 Cl H H H H CH₂CH₂CH₂OH H H O 0 A-4616 Cl H H H H CH₂CH(OH)CH₂CH₃ H H O 0 A-4617 Cl H H H H CH₂CH(OH)C(CH₃)₃ H H O 0 A-4618 Cl H H H H CH₂CH₂CH(OH)CH₃ H H O 0 A-4619 Cl H H H H CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-4620 Cl H H H H CH₂C(═NOH)CH₃ H H O 0 A-4621 Cl H H H H CH₂C(═NOH)CH₂CH₃ H H O 0 A-4622 Cl H H H H CH₂C(═NOH)C(CH₃)₃ H H O 0 A-4623 Cl H H H H CH₂C(═NOCH₃)CH₃ H H O 0 A-4624 Cl H H H H CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-4625 Cl H H H H CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-4626 Cl H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-4627 Cl H H H H CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-4628 Cl H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-4629 Cl H H H H CH₂Ph H H O 0 A-4630 Cl H H H H CH₂(2-F)Ph H H O 0 A-4631 Cl H H H H CH₂(3-F)Ph H H O 0

TABLE 77 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4632 Cl H H H H CH₂(4-F)Ph H H O 0 A-4633 Cl H H H H CH₂(2-Cl)Ph H H O 0 A-4634 Cl H H H H CH₂(3-Cl)Ph H H O 0 A-4635 Cl H H H H CH₂(4-Cl)Ph H H O 0 A-4636 Cl H H H H CH₂(2-CF₃)Ph H H O 0 A-4637 Cl H H H H CH₂(3-CF₃)Ph H H O 0 A-4638 Cl H H H H CH₂(4-CF₃)Ph H H O 0 A-4639 Cl H H H H CH₂(naphthalen-1-yl) H H O 0 A-4640 Cl H H H H CH₂(naphthalen-2-yl) H H O 0 A-4641 Cl H H H H CH₂CH₂Ph H H O 0 A-4642 H H H Cl H H H H O 0 A-4643 H H H Cl H CH₃ H H O 0 A-4644 H H H Cl H CH₂CH₃ H H O 0 A-4645 H H H Cl H CH(CH₃)₂ H H O 0 A-4646 H H H Cl H CH₂CH₂CH₃ H H O 0 A-4647 H H H Cl H CH₂CH(CH₃)₂ H H O 0 A-4648 H H H Cl H CH(CH₃)CH₂CH₃ H H O 0 A-4649 H H H Cl H CH₂C(CH₃)₃ H H O 0 A-4650 H H H Cl H CH₂(CH₂)₂CH₃ H H O 0 A-4651 H H H Cl H CH₂(CH₂)₃CH₃ H H O 0 A-4652 H H H Cl H CH₂(CH₂)₄CH₃ H H O 0 A-4653 H H H Cl H CH₂(CH₂)₆CH₃ H H O 0 A-4654 H H H Cl H CH₂OCH₃ H H O 0 A-4655 H H H Cl H CH₂OCH₂CH₃ H H O 0 A-4656 H H H Cl H CH₂CH₂OCH₃ H H O 0 A-4657 H H H Cl H CH₂CH₂OCH₂CH₃ H H O 0 A-4658 H H H Cl H CF₃ H H O 0 A-4659 H H H Cl H CHF₂ H H O 0 A-4660 H H H Cl H CH₂CF₃ H H O 0 A-4661 H H H Cl H CH₂CHF₂ H H O 0 A-4662 H H H Cl H CH₂CClF₂ H H O 0 A-4663 H H H Cl H CH₂CBrF₂ H H O 0 A-4664 H H H Cl H CF₂CF₃ H H O 0 A-4665 H H H Cl H CF₂CHF₂ H H O 0 A-4666 H H H Cl H CH₂CH₂CF₃ H H O 0 A-4667 H H H Cl H CH₂CF₂CF₃ H H O 0 A-4668 H H H Cl H CH₂CF₂CHF₂ H H O 0 A-4669 H H H Cl H CF₂CHFCF₃ H H O 0 A-4670 H H H Cl H CF₂CF₂CF₃ H H O 0 A-4671 H H H Cl H CH₂CF₂CF₂CF₃ H H O 0 A-4672 H H H Cl H CH₂CH₂CH₂CF₃ H H O 0 A-4673 H H H Cl H CH₂CH₂CF₂CF₃ H H O 0 A-4674 H H H Cl H CF₂CF₂CF₂CF₃ H H O 0 A-4675 H H H Cl H CH₂CH₂CH(CF₃)₂ H H O 0 A-4676 H H H Cl H CF₂CF₂CF₂CF₂CF₃ H H O 0 A-4677 H H H Cl H CH₂CF₂CF₂CF₂CF₃ H H O 0 A-4678 H H H Cl H CH₂CH₂CH₂CH₂CF₃ H H O 0 A-4679 H H H Cl H CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-4680 H H H Cl H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-4681 H H H Cl H CF₂CHFOCH₃ H H O 0 A-4682 H H H Cl H CF₂CHFOCH₂CH₃ H H O 0 A-4683 H H H Cl H CH₂CH₂OCH₂CF₃ H H O 0 A-4684 H H H Cl H CF₂CHFOCF₃ H H O 0 A-4685 H H H Cl H CF₂CHFOCF₂CF₃ H H O 0 A-4686 H H H Cl H CF₂CHFOCF₂CF₂CF₃ H H O 0 A-4687 H H H Cl H CH₂CH═CH₂ H H O 0 A-4688 H H H Cl H CH₂CH═CHCl H H O 0 A-4689 H H H Cl H CH₂CH═CCl₂ H H O 0 A-4690 H H H Cl H CH₂CH₂CF═CF₂ H H O 0 A-4691 H H H Cl H CH₂CH₂CH═CF₂ H H O 0 A-4692 H H H Cl H CH₂C≡CH H H O 0

TABLE 78 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4693 H H H Cl H CH₂C≡CCH₃ H H O 0 A-4694 H H H Cl H CH₂C≡CCF₃ H H O 0 A-4695 H H H Cl H CH₂C≡CI H H O 0 A-4696 H H H Cl H cyclobutyl H H O 0 A-4697 H H H Cl H cyclopentyl H H O 0 A-4698 H H H Cl H cyclohexyl H H O 0 A-4699 H H H Cl H 4,4-difluorocyclohexyl H H O 0 A-4700 H H H Cl H CH₂(cyclopropyl) H H O 0 A-4701 H H H Cl H CH₂(cyclobutyl) H H O 0 A-4702 H H H Cl H CH₂(cyclopentyl) H H O 0 A-4703 H H H Cl H CH₂CH₂(cyclopropyl) H H O 0 A-4704 H H H Cl H CH₂(2,2-difluororyclopropyl) H H O 0 A-4705 H H H Cl H CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4706 H H H Cl H CH₂(4,4-difluorocyclohexyl) H H O 0 A-4707 H H H Cl H CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-4708 H H H Cl H CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4709 H H H Cl H CH₂SCH₃ H H O 0 A-4710 H H H Cl H CH₂SCH₂CH₃ H H O 0 A-4711 H H H Cl H CH₂CH₂SCH₃ H H O 0 A-4712 H H H Cl H CH₂CH₂SCH₂CH₃ H H O 0 A-4713 H H H Cl H CH₂CH₂CH₂SCH₃ H H O 0 A-4714 H H H Cl H CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-4715 H H H Cl H CH(CH₃)SCH₃ H H O 0 A-4716 H H H Cl H CH(CH₃)SCH₂CH₃ H H O 0 A-4717 H H H Cl H CH₂CH(CH₃)SCH₃ H H O 0 A-4718 H H H Cl H CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4719 H H H Cl H CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-4720 H H H Cl H CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-4721 H H H Cl H CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-4722 H H H Cl H CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-4723 H H H Cl H CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-4724 H H H Cl H CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4725 H H H Cl H CH₂SOCH₃ H H O 0 A-4726 H H H Cl H CH₂CH₂SOCH₃ H H O 0 A-4727 H H H Cl H CH₂CH₂CH₂SOCH₃ H H O 0 A-4728 H H H Cl H CH(CH₃)SOCH₃ H H O 0 A-4729 H H H Cl H CH₂CH(CH₃)SOCH₃ H H O 0 A-4730 H H H Cl H CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-4731 H H H Cl H CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-4732 H H H Cl H CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-4733 H H H Cl H CH₂SO₂CH₃ H H O 0 A-4734 H H H Cl H CH₂CH₂SO₂CH₃ H H O 0 A-4735 H H H Cl H CH₂CH₂CH₂SO₂CH₃ H H O 0 A-4736 H H H Cl H CH(CH₃)SO₂CH₃ H H O 0 A-4737 H H H Cl H CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4738 H H H Cl H CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-4739 H H H Cl H CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-4740 H H H Cl H CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4741 H H H Cl H CH₂SCF₃ H H O 0 A-4742 H H H Cl H CH₂SCHF₂ H H O 0 A-4743 H H H Cl H CH₂SCH₂CF₃ H H O 0 A-4744 H H H Cl H CH₂SCH₂CHF₂ H H O 0 A-4745 H H H Cl H CH₂SCF₂CF₃ H H O 0 A-4746 H H H Cl H CH₂CH₂SCF₃ H H O 0 A-4747 H H H Cl H CH₂CH₂SCH₂CF₃ H H O 0 A-4748 H H H Cl H CH₂CH₂CH₂SCF₃ H H O 0 A-4749 H H H Cl H CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-4750 H H H Cl H CH(CH₃)SCF₃ H H O 0 A-4751 H H H Cl H CH(CH₃)SCH₂CF₃ H H O 0 A-4752 H H H Cl H CH₂CH(CH₃)SCF₃ H H O 0 A-4753 H H H Cl H CH₂CH(CH₃)SCH₂CF₃ H H O 0

TABLE 79 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4754 H H H Cl H CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-4755 H H H Cl H CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-4756 H H H Cl H CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-4757 H H H Cl H CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-4758 H H H Cl H CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-4759 H H H Cl H CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4760 H H H Cl H CH₂SOCF₃ H H O 0 A-4761 H H H Cl H CH₂CH₂SOCF₃ H H O 0 A-4762 H H H Cl H CH₂CH₂CH₂SOCF₃ H H O 0 A-4763 H H H Cl H CH(CH₃)SOCF₃ H H O 0 A-4764 H H H Cl H CH₂CH(CH₃)SOCF₃ H H O 0 A-4765 H H H Cl H CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-4766 H H H Cl H CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-4767 H H H Cl H CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-4768 H H H Cl H CH₂SO₂CF₃ H H O 0 A-4769 H H H Cl H CH₂CH₂SO₂CF₃ H H O 0 A-4770 H H H Cl H CH₂CH₂CH₂SO₂CF₃ H H O 0 A-4771 H H H Cl H CH(CH₃)SO₂CF₃ H H O 0 A-4772 H H H CI H CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4773 H H H Cl H CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-4774 H H H Cl H CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-4775 H H H Cl H CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4776 H H H Cl H CH₂C(═O)CH₃ H H O 0 A-4777 H H H Cl H CH₂C(═O)CH₂CH₃ H H O 0 A-4778 H H H Cl H CH₂C(═O)C(CH₃)₃ H H O 0 A-4779 H H H Cl H CH₂CH₂C(═O)CH₃ H H O 0 A-4780 H H H Cl H CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-4781 H H H Cl H CH₂C(═O)CF₃ H H O 0 A-4782 H H H Cl H CH₂CH₂C(═O)CF₃ H H O 0 A-4783 H H H Cl H CH₂C(═O)OCH₃ H H O 0 A-4784 H H H Cl H CH₂C(═O)OCH₂CH₃ H H O 0 A-4785 H H H Cl H CH₂C(═O)OC(CH₃)₃ H H O 0 A-4786 H H H Cl H CH₂CH₂C(═O)OCH₃ H H O 0 A-4787 H H H Cl H CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-4788 H H H Cl H CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-4789 H H H Cl H CH₂C(═O)NH₂ H H O 0 A-4790 H H H Cl H CH₂CH₂C(═O)NH₂ H H O 0 A-4791 H H H Cl H CH₂C(═O)NHCH₃ H H O 0 A-4792 H H H Cl H CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4793 H H H Cl H CH₂CH₂C(═O)NHCH₃ H H O 0 A-4794 H H H Cl H CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4795 H H H Cl H CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4796 H H H Cl H CH₂C(═C)NHCH₂CF₃ H H O 0 A-4797 H H H Cl H CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4798 H H H Cl H CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-4799 H H H Cl H CH₂C(═O)N(CH₃)₂ H H O 0 A-4800 H H H Cl H CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4801 H H H Cl H CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-4802 H H H Cl H CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4803 H H H Cl H CH₂CH₂OH H H O 0 A-4804 H H H Cl H CH₂CH(OH)CH₃ H H O 0 A-4805 H H H Cl H CH₂CH₂CH₂OH H H O 0 A-4806 H H H Cl H CH₂CH(OH)CH₂CH₃ H H O 0 A-4807 H H H Cl H CH₂CH(OH)C(CH₃)₃ H H O 0 A-4808 H H H Cl H CH₂CH₂CH(OH)CH₃ H H O 0 A-4809 H H H Cl H CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-4810 H H H Cl H CH₂C(═NOH)CH₃ H H O 0 A-4811 H H H Cl H CH₂C(═NOH)CH₂CH₃ H H O 0 A-4812 H H H Cl H CH₂C(═NOH)C(CH₃)₃ H H O 0 A-4813 H H H Cl H CH₂C(═NOCH₃)CH₃ H H O 0 A-4814 H H H Cl H CH₂C(═NOCH₃)CH₂CH₃ H H O 0

TABLE 80 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4815 H H H Cl H CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-4816 H H H Cl H CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-4817 H H H Cl H CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-4818 H H H Cl H CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-4819 H H H Cl H CH₂Ph H H O 0 A-4820 H H H Cl H CH₂(2-F)Ph H H O 0 A-4821 H H H Cl H CH₂(3-F)Ph H H O 0 A-4822 H H H Cl H CH₂(4-F)Ph H H O 0 A-4823 H H H Cl H CH₂(2-Cl)Ph H H O 0 A-4824 H H H Cl H CH₂(3-Cl)Ph H H O 0 A-4825 H H H Cl H CH₂(4-Cl)Ph H H O 0 A-4826 H H H Cl H CH₂(2-CF₃)Ph H H O 0 A-4827 H H H Cl H CH₂(3-CF₃)Ph H H O 0 A-4828 H H H Cl H CH₂(4-CF₃)Ph H H O 0 A-4829 H H H Cl H CH₂(naphthalen-1-yl) H H O 0 A-4830 H H H Cl H CH₂(naphthalen-2-yl) H H O 0 A-4831 H H H Cl H CH₂CH₂Ph H H O 0 A-4832 H H H H Cl H H H O 0 A-4833 H H H H Cl CH₃ H H O 0 A-4834 H H H H Cl CH₂CH₃ H H O 0 A-4835 H H H H Cl CH(CH₃)₂ H H O 0 A-4836 H H H H Cl CH₂CH₂CH₃ H H O 0 A-4837 H H H H Cl CH₂CH(CH₃)₂ H H O 0 A-4838 H H H H Cl CH(CH₃)CH₂CH₃ H H O 0 A-4839 H H H H Cl CH₂C(CH₃)₃ H H O 0 A-4840 H H H H Cl CH₂(CH₂)₂CH₃ H H O 0 A-4841 H H H H Cl CH₂(CH₂)₃CH₃ H H O 0 A-4842 H H H H Cl CH₂(CH₂)₄CH₃ H H O 0 A-4843 H H H H Cl CH₂(CH₂)₆CH₃ H H O 0 A-4844 H H H H Cl CH₂OCH₃ H H O 0 A-4845 H H H H Cl CH₂OCH₂CH₃ H H O 0 A-4846 H H H H Cl CH₂CH₂OCH₃ H H O 0 A-4847 H H H H Cl CH₂CH₂OCH₂CH₃ H H O 0 A-4848 H H H H Cl CF₃ H H O 0 A-4849 H H H H Cl CHF₂ H H O 0 A-4850 H H H H Cl CH₂CF₃ H H O 0 A-4851 H H H H Cl CH₂CHF₂ H H O 0 A-4852 H H H H Cl CH₂CClF₂ H H O 0 A-4853 H H H H Cl CH₂CBrF₂ H H O 0 A-4854 H H H H Cl CF₂CF₃ H H O 0 A-4855 H H H H Cl CF₂CHF₂ H H O 0 A-4856 H H H H Cl CH₂CH₂CF₃ H H O 0 A-4857 H H H H Cl CH₂CF₂CF₃ H H O 0 A-4858 H H H H Cl CH₂CF₂CHF₂ H H O 0 A-4859 H H H H Cl CF₂CHFCF₃ H H O 0 A-4860 H H H H Cl CF₂CF₂CF₃ H H O 0 A-4861 H H H H Cl CH₂CF₂CF₂CF₃ H H O 0 A-4862 H H H H Cl CH₂CH₂CH₂CF₃ H H O 0 A-4863 H H H H Cl CH₂CH₂CF₂CF₃ H H O 0 A-4864 H H H H Cl CF₂CF₂CF₂CF₃ H H O 0 A-4865 H H H H Cl CH₂CH₂CH(CF₃)₂ H H O 0 A-4866 H H H H Cl CF₂CF₂CF₂CF₂CF₃ H H O 0 A-4867 H H H H Cl CH₂CF₂CF₂CF₂CF₃ H H O 0 A-4868 H H H H Cl CH₂CH₂CH₂CH₂CF₃ H H O 0 A-4869 H H H H Cl CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-4870 H H H H Cl CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-4871 H H H H Cl CF₂CHFOCH₃ H H O 0 A-4872 H H H H Cl CF₂CHFOCH₂CH₃ H H O 0 A-4873 H H H H Cl CH₂CH₂OCH₂CF₃ H H O 0 A-4874 H H H H Cl CF₂CHFOCF₃ H H O 0 A-4875 H H H H Cl CF₂CHFOCF₂CF₃ H H O 0

TABLE 81 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4876 H H H H Cl CF₂CHFOCF₂CF₂CF₃ H H O 0 A-4877 H H H H Cl CH₂CH═CH₂ H H O 0 A-4878 H H H H Cl CH₂CH═CHCl H H O 0 A-4879 H H H H Cl CH₂CH═CCl₂ H H O 0 A-4880 H H H H Cl CH₂CH₂CF═CF₂ H H O 0 A-4881 H H H H Cl CH₂CH₂CH═CF₂ H H O 0 A-4882 H H H H Cl CH₂C≡CH H H O 0 A-4883 H H H H Cl CH₂C≡CCH₃ H H O 0 A-4884 H H H H Cl CH₂C≡CCF₃ H H O 0 A-4885 H H H H Cl CH₂C≡CI H H O 0 A-4886 H H H H Cl cyclobutyl H H O 0 A-4887 H H H H Cl cyclopentyl H H O 0 A-4888 H H H H Cl cyclohexyl H H O 0 A-4889 H H H H Cl 4,4-difluorocyclohexyl H H O 0 A-4890 H H H H Cl CH₂(cyclopropyl) H H O 0 A-4891 H H H H Cl CH₂(cyclobutyl) H H O 0 A-4892 H H H H Cl CH₂(cyclopentyl) H H O 0 A-4893 H H H H Cl CH₂CH₂(cyclopropyl) H H O 0 A-4894 H H H H Cl CH₂(2,2-difluorocyclopropyl) H H O 0 A-4895 H H H H Cl CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4896 H H H H Cl CH₂(4,4-difluorocyclohexyl) H H O 0 A-4897 H H H H Cl CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-4898 H H H H Cl CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-4899 H H H H Cl CH₂SCH₃ H H O 0 A-4900 H H H H Cl CH₂SCH₂CH₃ H H O 0 A-4901 H H H H Cl CH₂CH₂SCH₃ H H O 0 A-4902 H H H H Cl CH₂CH₂SCH₂CH₃ H H O 0 A-4903 H H H H Cl CH₂CH₂CH₂SCH₃ H H O 0 A-4904 H H H H Cl CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-4905 H H H H Cl CH(CH₃)SCH₃ H H O 0 A-4906 H H H H Cl CH(CH₃)SCH₂CH₃ H H O 0 A-4907 H H H H Cl CH₂CH(CH₃)SCH₃ H H O 0 A-4908 H H H H Cl CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4909 H H H H Cl CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-4910 H H H H Cl CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-4911 H H H H Cl CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-4912 H H H H Cl CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-4913 H H H H Cl CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-4914 H H H H Cl CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-4915 H H H H Cl CH₂SOCH₃ H H O 0 A-4916 H H H H Cl CH₂CH₂SOCH₃ H H O 0 A-4917 H H H H Cl CH₂CH₂CH₂SOCH₃ H H O 0 A-4918 H H H H Cl CH(CH₃)SOCH₃ H H O 0 A-4919 H H H H Cl CH₂CH(CH₃)SOCH₃ H H O 0 A-4920 H H H H Cl CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-4921 H H H H Cl CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-4922 H H H H Cl CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-4923 H H H H Cl CH₂SO₂CH₃ H H O 0 A-4924 H H H H Cl CH₂CH₂SO₂CH₃ H H O 0 A-4925 H H H H Cl CH₂CH₂CH₂SO₂CH₃ H H O 0 A-4926 H H H H Cl CH(CH₃)SO₂CH₃ H H O 0 A-4927 H H H H Cl CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4928 H H H H Cl CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-4929 H H H H Cl CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-4930 H H H H Cl CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-4931 H H H H Cl CH₂SCF₃ H H O 0 A-4932 H H H H Cl CH₂SCHF₂ H H O 0 A-4933 H H H H Cl CH₂SCH₂CF₃ H H O 0 A-4934 H H H H Cl CH₂SCH₂CHF₂ H H O 0 A-4935 H H H H Cl CH₂SCF₂CF₃ H H O 0 A-4936 H H H H Cl CH₂CH₂SCF₃ H H O 0

TABLE 82 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4937 H H H H Cl CH₂CH₂SCH₂CF₃ H H O 0 A-4938 H H H H Cl CH₂CH₂CH₂SCF₃ H H O 0 A-4939 H H H H Cl CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-4940 H H H H Cl CH(CH₃)SCF₃ H H O 0 A-4941 H H H H Cl CH(CH₃)SCH₂CF₃ H H O 0 A-4942 H H H H Cl CH₂CH(CH₃)SCF₃ H H O 0 A-4943 H H H H Cl CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4944 H H H H Cl CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-4945 H H H H Cl CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-4946 H H H H Cl CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-4947 H H H H Cl CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-4948 H H H H Cl CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-4949 H H H H Cl CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-4950 H H H H Cl CH₂SOCF₃ H H O 0 A-4951 H H H H Cl CH₂CH₂SOCF₃ H H O 0 A-4952 H H H H Cl CH₂CH₂CH₂SOCF₃ H H O 0 A-4953 H H H H Cl CH(CH₃)SOCF₃ H H O 0 A-4954 H H H H Cl CH₂CH(CH₃)SOCF₃ H H O 0 A-4955 H H H H Cl CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-4956 H H H H Cl CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-4957 H H H H Cl CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-4958 H H H H Cl CH₂SO₂CF₃ H H O 0 A-4959 H H H H Cl CH₂CH₂SO₂CF₃ H H O 0 A-4960 H H H H Cl CH₂CH₂CH₂SO₂CF₃ H H O 0 A-4961 H H H H Cl CH(CH₃)SC₂CF₃ H H O 0 A-4962 H H H H Cl CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4963 H H H H Cl CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-4964 H H H H Cl CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-4965 H H H H Cl CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0 A-4966 H H H H Cl CH₂C(═O)CH₃ H H O 0 A-4967 H H H H Cl CH₂C(═O)CH₂CH₃ H H O 0 A-4968 H H H H Cl CH₂C(═O)C(CH₃)₃ H H O 0 A-4969 H H H H Cl CH₂CH₂C(═O)CH₃ H H O 0 A-4970 H H H H Cl CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-4971 H H H H Cl CH₂C(═O)CF₃ H H O 0 A-4972 H H H H Cl CH₂CH₂C(═O)CF₃ H H O 0 A-4973 H H H H Cl CH₂C(═O)OCH₃ H H O 0 A-4974 H H H H Cl CH₂C(═O)OCH₂CH₃ H H O 0 A-4975 H H H H Cl CH₂C(═O)OC(CH₃)₃ H H O 0 A-4976 H H H H Cl CH₂CH₂C(═O)OCH₃ H H O 0 A-4977 H H H H Cl CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-4978 H H H H Cl CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-4979 H H H H Cl CH₂C(═O)NH₂ H H O 0 A-4980 H H H H Cl CH₂CH₂C(═O)NH₂ H H O 0 A-4981 H H H H Cl CH₂C(═O)NHCH₃ H H O 0 A-4982 H H H H Cl CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4983 H H H H Cl CH₂CH₂C(═O)NHCH₃ H H O 0 A-4984 H H H H Cl CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-4985 H H H H Cl CH₂C(═O)NHCH₂CHF₂ H H O 0 A-4986 H H H H Cl CH₂C(═O)NHCH₂CF₃ H H O 0 A-4987 H H H H Cl CH₂CH₂C( ═O)NHCH₂CHF₂ H H O 0 A-4988 H H H H Cl CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-4989 H H H H Cl CH₂C(═O)N(CH₃)₂ H H O 0 A-4990 H H H H Cl CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4991 H H H H Cl CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-4992 H H H H Cl CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-4993 H H H H Cl CH₂CH₂OH H H O 0 A-4994 H H H H Cl CH₂CH(OH)CH₃ H H O 0 A-4995 H H H H Cl CH₂CH₂CH₂OH H H O 0 A-4996 H H H H Cl CH₂CH(OH)CH₂CH₃ H H O 0 A-4997 H H H H Cl CH₂CH(OH)C(CH₃)₃ H H O 0

TABLE 83 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-4998 H H H H Cl CH₂CH₂CH(OH)CH₃ H H O 0 A-4999 H H H H Cl CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-5000 H H H H Cl CH₂C(═NOH)CH₃ H H O 0 A-5001 H H H H Cl CH₂C(═NOH)CH₂CH₃ H H O 0 A-5002 H H H H Cl CH₂C(═NOH)C(CH₃)₃ H H O 0 A-5003 H H H H Cl CH₂C(═NOCH₃)CH₃ H H O 0 A-5004 H H H H Cl CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-5005 H H H H Cl CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-5006 H H H H Cl CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-5007 H H H H Cl CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-5008 H H H H Cl CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-5009 H H H H Cl CH₂Ph H H O 0 A-5010 H H H H Cl CH₂(2-F)Ph H H O 0 A-5011 H H H H Cl CH₂(3-F)Ph H H O 0 A-5012 H H H H Cl CH₂(4-F)Ph H H O 0 A-5013 H H H H Cl CH₂(2-Cl)Ph H H O 0 A-5014 H H H H Cl CH₂(3-Cl)Ph H H O 0 A-5015 H H H H Cl CH₂(4-Cl)Ph H H O 0 A-5016 H H H H Cl CH₂(2-CF₃)Ph H H O 0 A-5017 H H H H Cl CH₂(3-CF₃)Ph H H O 0 A-5018 H H H H Cl CH₂(4-CF₃)Ph H H O 0 A-5019 H H H H Cl CH₂(naphthalen-1-yl) H H O 0 A-5020 H H H H Cl CH₂(naphthalen-2-yl) H H O 0 A-5021 H H H H Cl CH₂CH₂Ph H H O 0 A-5022 H H H H F H H H O 0 A-5023 H H H H F CH₃ H H O 0 A-5024 H H H H F CH₂CH₃ H H O 0 A-5025 H H H H F CH(CH₃)₂ H H O 0 A-5026 H H H H F CH₂CH₂CH₃ H H O 0 A-5027 H H H H F CH₂CH(CH₃)₂ H H O 0 A-5028 H H H H F CH(CH₃)CH₂CH₃ H H O 0 A-5029 H H H H F CH₂C(CH₃)₃ H H O 0 A-5030 H H H H F CH₂(CH₂)₂CH₃ H H O 0 A-5031 H H H H F CH₂(CH₂)₃CH₃ H H O 0 A-5032 H H H H F CH₂(CH₂)₄CH₃ H H O 0 A-5033 H H H H F CH₂(CH₂)₆CH₃ H H O 0 A-5034 H H H H F CH₂OCH₃ H H O 0 A-5035 H H H H F CH₂OCH₂CH₃ H H O 0 A-5036 H H H H F CH₂CH₂OCH₃ H H O 0 A-5037 H H H H F CH₂CH₂OCH₂CH₃ H H O 0 A-5038 H H H H F CF₃ H H O 0 A-5039 H H H H F CHF₂ H H O 0 A-5040 H H H H F CH₂CF₃ H H O 0 A-5041 H H H H F CH₂CHF₂ H H O 0 A-5042 H H H H F CH₂CClF₂ H H O 0 A-5043 H H H H F CH₂CBrF₂ H H O 0 A-5044 H H H H F CF₂CF₃ H H O 0 A-5045 H H H H F CF₂CHF₂ H H O 0 A-5046 H H H H F CH₂CH₂CF₃ H H O 0 A-5047 H H H H F CH₂CF₂CF₃ H H O 0 A-5048 H H H H F CH₂CF₂CHF₂ H H O 0 A-5049 H H H H F CF₂CHFCF₃ H H O 0 A-5050 H H H H F CF₂CF₂CF₃ H H O 0 A-5051 H H H H F CH₂CF₂CF₂CF₃ H H O 0 A-5052 H H H H F CH₂CH₂CH₂CF₃ H H O 0 A-5053 H H H H F CH₂CH₂CF₂CF₃ H H O 0 A-5054 H H H H F CF₂CF₂CF₂CF₃ H H O 0 A-5055 H H H H F CH₂CH₂CH(CF₃)₂ H H O 0 A-5056 H H H H F CF₂CF₂CF₂CF₂CF₃ H H O 0 A-5057 H H H H F CH₂CF₂CF₂CF₂CF₃ H H O 0 A-5058 H H H H F CH₂CH₂CH₂CH₂CF₃ H H O 0

TABLE 84 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5059 H H H H F CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-5060 H H H H F CH₂CF₂CF(CF₃)CF₂C(CF₂)₃ H H O 0 A-5061 H H H H F CF₂CHFOCH₃ H H O 0 A-5062 H H H H F CF₂CHFOCH₂CH₃ H H O 0 A-5063 H H H H F CH₂CH₂OCH₂CF₃ H H O 0 A-5064 H H H H F CF₂CHFOCF₃ H H O 0 A-5065 H H H H F CF₂CHFOCF₂CF₃ H H O 0 A-5066 H H H H F CF₂CHFOCF₂CF₂CF₃ H H O 0 A-5067 H H H H F CH₂CH═CH₂ H H O 0 A-5068 H H H H F CH₂CH═CHCl H H O 0 A-5069 H H H H F CH₂CH═CCl₂ H H O 0 A-5070 H H H H F CH₂CH₂CF═CF₂ H H O 0 A-5071 H H H H F CH₂CH₂CH═CF₂ H H O 0 A-5072 H H H H F CH₂C≡CH H H O 0 A-5073 H H H H F CH₂C≡CCH₃ H H O 0 A-5074 H H H H F CH₂C≡CCF₃ H H O 0 A-5075 H H H H F CH₂C≡CI H H O 0 A-5076 H H H H F cyclobutyl H H O 0 A-5077 H H H H F cyclopentyl H H O 0 A-5078 H H H H F cyclohexyl H H O 0 A-5079 H H H H F 4,4-difluorocyclohexyl H H O 0 A-5080 H H H H F CH₂(cyclopropyl) H H O 0 A-5081 H H H H F CH₂(cyclobutyl) H H O 0 A-5082 H H H H F CH₂(cyclopentyl) H H O 0 A-5083 H H H H F CH₂CH₂(cyclopropyl) H H O 0 A-5084 H H H H F CH₂(2,2-difluorocyclopropyl) H H O 0 A-5085 H H H H F CH₂(2,2-dichlorocyclopropyl) H H O 0 A-5086 H H H H F CH₂(4,4-difluorocyclohexyl) H H O 0 A-5087 H H H H F CH₂CH₂(2,2-difluorocyclcpropyl) H H O 0 A-5088 H H H H F CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-5089 H H H H F CH₂SCH₃ H H O 0 A-5090 H H H H F CH₂SCH₂CH₃ H H O 0 A-5091 H H H H F CH₂CH₂SCH₃ H H O 0 A-5092 H H H H F CH₂CH₂SCH₂CH₃ H H O 0 A-5093 H H H H F CH₂CH₂CH₂SCH₃ H H O 0 A-5094 H H H H F CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-5095 H H H H F CH(CH₃)SCH₃ H H O 0 A-5096 H H H H F CH(CH₃)SCH₂CH₃ H H O 0 A-5097 H H H H F CH₂CH(CH₃)SCH₃ H H O 0 A-5098 H H H H F CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-5099 H H H H F CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-5100 H H H H F CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-5101 H H H H F CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-5102 H H H H F CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-5103 H H H H F CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-5104 H H H H F CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-5105 H H H H F CH₂SOCH₃ H H O 0 A-5106 H H H H F CH₂CH₂SOCH₃ H H O 0 A-5107 H H H H F CH₂CH₂CH₂SOCH₃ H H O 0 A-5108 H H H H F CH(CH₃)SOCH₃ H H O 0 A-5109 H H H H F CH₂CH(CH₃)SOCH₃ H H O 0 A-5110 H H H H F CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-5111 H H H H F CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-5112 H H H H F CH₂CH₂CH(CH₃)SOCH₃ H H O 0 A-5113 H H H H F CH₂SO₂CH₃ H H O 0 A-5114 H H H H F CH₂CH₂SO₂CH₃ H H O 0 A-5115 H H H H F CH₂CH₂CH₂SO₂CH₃ H H O 0 A-5116 H H H H F CH(CH₃)SO₂CH₃ H H O 0 A-5117 H H H H F CH₂CH(CH₃)SO₂CH₃ H H O 0 A-5118 H H H H F CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-5119 H H H H F CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0

TABLE 85 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5120 H H H H F CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-5121 H H H H F CH₂SCF₃ H H O 0 A-5122 H H H H F CH₂SCHF₂ H H O 0 A-5123 H H H H F CH₂SCH₂CF₃ H H O 0 A-5124 H H H H F CH₂SCH₂CHF₂ H H O 0 A-5125 H H H H F CH₂SCF₂CF₃ H H O 0 A-5126 H H H H F CH₂CH₂SCF₃ H H O 0 A-5127 H H H H F CH₂CH₂SCH₂CF₃ H H O 0 A-5128 H H H H F CH₂CH₂CH₂SCF₃ H H O 0 A-5129 H H H H F CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-5130 H H H H F CH(CH₃)SCF₃ H H O 0 A-5131 H H H H F CH(CH₃)SCH₂CF₃ H H O 0 A-5132 H H H H F CH₂CH(CH₃)SCF₃ H H O 0 A-5133 H H H H F CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-5134 H H H H F CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-5135 H H H H F CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-5136 H H H H F CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-5137 H H H H F CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-5138 H H H H F CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-5139 H H H H F CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-5140 H H H H F CH₂SOCF₃ H H O 0 A-5141 H H H H F CH₂CH₂SOCF₃ H H O 0 A-5142 H H H H F CH₂CH₂CH₂SOCF₃ H H O 0 A-5143 H H H H F CH(CH₃)SOCF₃ H H O 0 A-5144 H H H H F CH₂CH(CH₃)SOCF₃ H H O 0 A-5145 H H H H F CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-5146 H H H H F CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-5147 H H H H F CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-5148 H H H H F CH₂SO₂CF₃ H H O 0 A-5149 H H H H F CH₂CH₂SO₂CF₃ H H O 0 A-5150 H H H H F CH₂CH₂CH₂SO₂CF₃ H H O 0 A-5151 H H H H F CH(CH₃)SO₂CF₃ H H O 0 A-5152 H H H H F CH₂CH(CH₃)SO₂CF₃ H H O 0 A-5153 H H H H F CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-5154 H H H H F CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-5155 H H H H F CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0 A-5156 H H H H F CH₂C(═O)CH₃ H H O 0 A-5157 H H H H F CH₂C(═O)CH₂CH₃ H H O 0 A-5158 H H H H F CH₂C(═O)C(CH₃)₃ H H O 0 A-5159 H H H H F CH₂CH₂C(═O)CH₃ H H O 0 A-5160 H H H H F CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-5161 H H H H F CH₂C(═O)CF₃ H H O 0 A-5162 H H H H F CH₂CH₂C(═O)CF₃ H H O 0 A-5163 H H H H F CH₂C(═O)OCH₃ H H O 0 A-5164 H H H H F CH₂C(═O)OCH₂CH₃ H H O 0 A-5165 H H H H F CH₂C(═O)OC(CH₃)₃ H H O 0 A-5166 H H H H F CH₂CH₂C(═O)OCH₃ H H O 0 A-5167 H H H H F CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-5168 H H H H F CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-5169 H H H H F CH₂C(═O)NH₂ H H O 0 A-5170 H H H H F CH₂CH₂C(═O)NH₂ H H O 0 A-5171 H H H H F CH₂C(═O)NHCH₃ H H O 0 A-5172 H H H H F CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-5173 H H H H F CH₂CH₂C(═O)NHCH₃ H H O 0 A-5174 H H H H F CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-5175 H H H H F CH₂C(═O)NHCH₂CHF₂ H H O 0 A-5176 H H H H F CH₂C(═O)NHCH₂CF₃ H H O 0 A-5177 H H H H F CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-5178 H H H H F CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-5179 H H H H F CH₂C(═O)N(CH₃)₂ H H O 0 A-5180 H H H H F CH₂C(═O)N(CH₂CH₃)₂ H H O 0

TABLE 86 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5181 H H H H F CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-5182 H H H H F CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-5183 H H H H F CH₂CH₂OH H H O 0 A-S184 H H H H F CH₂CH(OH)CH₃ H H O 0 A-5185 H H H H F CH₂CH₂CH₂OH H H O 0 A-5186 H H H H F CH₂CH(OH)CH₂CH₃ H H O 0 A-5187 H H H H F CH₂CH(OH)C(CH₃)₃ H H O 0 A-5188 H H H H F CH₂CH₂CH(OH)CH₃ H H O 0 A-5189 H H H H F CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-5190 H H H H F CH₂C(═NOH)CH₃ H H O 0 A-5191 H H H H F CH₂C(═NOH)CH₂CH₃ H H O 0 A-5192 H H H H F CH₂C(═NOH)C(CH₃)₃ H H O 0 A-5193 H H H H F CH₂C(═NOCH₃)CH₃ H H O 0 A-5194 H H H H F CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-5195 H H H H F CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-5196 H H H H F CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-5197 H H H H F CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-5198 H H H H F CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-5199 H H H H F CH₂Ph H H O 0 A-5200 H H H H F CH₂(2-F)Ph H H O 0 A-5201 H H H H F CH₂(3-F)Ph H H O 0 A-5202 H H H H F CH₂(4-F)Ph H H O 0 A-5203 H H H H F CH₂(2-Cl)Ph H H O 0 A-5204 H H H H F CH₂(3-Cl)Ph H H O 0 A-5205 H H H H F CH₂(4-Cl)Ph H H O 0 A-520S H H H H F CH₂(2-CF₃)Ph H H O 0 A-5207 H H H H F CH₂(3-CF₃)Ph H H O 0 A-5208 H H H H F CH₂(4-CF₃)Ph H H O 0 A-5209 H H H H F CH₂(naphthalen-1-yl) H H O 0 A-5210 H H H H F CH₂(naphthalen-2-yl) H H O 0 A-5211 H H H H F CH₂CH₂Ph H H O 0 A-5212 H H H H CH₃ H H H O 0 A-5213 H H H H CH₃ CH₃ H H O 0 A-5214 H H H H CH₃ CH₂CH₃ H H O 0 A-5215 H H H H CH₃ CH(CH₃)₂ H H O 0 A-5216 H H H H CH₃ CH₂CH₂CH₃ H H O 0 A-5217 H H H H CH₃ CH₂CH(CH₃)₂ H H O 0 A-5218 H H H H CH₃ CH(CH₃)CH₂CH₂ H H O 0 A-5219 H H H H CH₃ CH₂C(CH₃)₃ H H O 0 A-5220 H H H H CH₃ CH₂(CH₂)₂CH₃ H H O 0 A-5221 H H H H CH₃ CH₂(CH₂)₃CH₃ H H O 0 A-5222 H H H H CH₃ CH₂(CH₂)₄CH₃ H H O 0 A-5223 H H H H CH₃ CH₂(CH₂)₆CH₃ H H O 0 A-5224 H H H H CH₃ CH₂OCH₃ H H O 0 A-5225 H H H H CH₃ CH₂OCH₂CH₃ H H O 0 A-5226 H H H H CH₃ CH₂CH₂OCH₃ H H O 0 A-5227 H H H H CH₃ CH₂CH₂OCH₂CH₃ H H O 0 A-5228 H H H H CH₃ CF₃ H H O 0 A-5229 H H H H CH₃ CHF₂ H H O 0 A-5230 H H H H CH₃ CH₂CF₃ H H O 0 A-5231 H H H H CH₃ CH₂CHF₂ H H O 0 A-5232 H H H H CH₃ CH₂CClF₂ H H O 0 A-5233 H H H H CH₃ CH₂CBrF₂ H H O 0 A-5234 H H H H CH₃ CF₂CF₃ H H O 0 A-5235 H H H H CH₃ CF₂CHF₂ H H O 0 A-5236 H H H H CH₃ CH₂CH₂CF₃ H H O 0 A-5237 H H H H CH₃ CH₂CF₂CF₃ H H O 0 A-5238 H H H H CH₃ CH₂CF₂CHF₂ H H O 0 A-5239 H H H H CH₃ CF₂CHFCF₃ H H O 0 A-5240 H H H H CH₃ CF₂CF₂CF₃ H H O 0 A-5241 H H H H CH₃ CH₂CF₂CF₂CF₃ H H O 0

TABLE 87 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5242 H H H H CH₃ CH₂CH₂CH₂CF₃ H H O 0 A-5243 H H H H CH₃ CH₂CH₂CF₂CF₃ H H O 0 A-5244 H H H H CH₃ CF₂CF₂CF₂CF₃ H H O 0 A-5245 H H H H CH₃ CH₂CH₂CH(CF₃)₂ H H O 0 A-5246 H H H H CH₃ CF₂CF₂CF₂CF₂CF₃ H H O 0 A-5247 H H H H CH₃ CH₂CF₂CF₂CF₂CF₃ H H O 0 A-5248 H H H H CH₃ CH₂CH₂CH₂CH₂CF₃ H H O 0 A-5249 H H H H CH₃ CH₂CF₂CF₂CF₂CHF₂ H H O 0 A-5250 H H H H CH₃ CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 0 A-5251 H H H H CH₃ CF₂CHFOCH₃ H H O 0 A-5252 H H H H CH₃ CF₂CHFOCH₂CH₃ H H O 0 A-5253 H H H H CH₃ CH₂CH₂OCH₂CF₃ H H O 0 A-S254 H H H H CH₃ CF₂CHFOCF₃ H H O 0 A-5255 H H H H CH₃ CF₂CHFOCF₂CF₃ H H O 0 A-5256 H H H H CH₃ CF₂CHFOCF₂CF₂CF₃ H H O 0 A-5257 H H H H CH₃ CH₂CH═CH₂ H H O 0 A-5258 H H H H CH₃ CH₂CH═CHCl H H O 0 A-5259 H H H H CH₃ CH₂CH═CCl₂ H H O 0 A-5260 H H H H CH₃ CH₂CH₂CF═CF₂ H H O 0 A-5261 H H H H CH₃ CH₂CH₂CH═CF₂ H H O 0 A-5262 H H H H CH₃ CH₂C≡CH H H O 0 A-5263 H H H H CH₃ CH₂C≡CCH₃ H H O 0 A-5264 H H H H CH₃ CH₂C≡CCF₃ H H O 0 A-5265 H H H H CH₃ CH₂C≡CI H H O 0 A-5266 H H H H CH₃ cyclobutyl H H O 0 A-5267 H H H H CH₃ cyclopentyl H H O 0 A-5268 H H H H CH₃ cyclohexyl H H O 0 A-5269 H H H H CH₃ 4,4-difluorocyclohexyl H H O 0 A-5270 H H H H CH₃ CH₂(cyclopropyl) H H O 0 A-5271 H H H H CH₃ CH₂(cyclobutyl) H H O 0 A-5272 H H H H CH₃ CH₂(cyclopentyl) H H O 0 A-5273 H H H H CH₃ CH₂CH₂(cyclopropyl) H H O 0 A-5274 H H H H CH₃ CH₂(2,2-difluorocyclopropyl) H H O 0 A-5275 H H H H CH₃ CH₂(2,2-dichlorocyclopropyl) H H O 0 A-5276 H H H H CH₃ CH₂(4,4-difluorocyclohexyl) H H O 0 A-5277 H H H H CH₃ CH₂CH₂(2,2-difluorocyclopropyl) H H O 0 A-5278 H H H H CH₃ CH₂CH₂(2,2-dichlorocyclopropyl) H H O 0 A-5279 H H H H CH₃ CH₂SCH₃ H H O 0 A-5280 H H H H CH₃ CH₂SCH₂CH₃ H H O 0 A-5281 H H H H CH₃ CH₂CH₂SCH₃ H H O 0 A-5282 H H H H CH₃ CH₂CH₂SCH₂CH₃ H H O 0 A-5283 H H H H CH₃ CH₂CH₂CH₂SCH₃ H H O 0 A-5284 H H H H CH₃ CH₂CH₂CH₂SCH₂CH₃ H H O 0 A-5285 H H H H CH₃ CH(CH₃)SCH₃ H H O 0 A-5286 H H H H CH₃ CH(CH₃)SCH₂CH₃ H H O 0 A-5287 H H H H CH₃ CH₂CH(CH₃)SCH₃ H H O 0 A-5288 H H H H CH₃ CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-5289 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₃ H H O 0 A-5290 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 0 A-5291 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₃ H H O 0 A-5292 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 0 A-5293 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₃ H H O 0 A-5294 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 0 A-5295 H H H H CH₃ CH₂SOCH₃ H H O 0 A-5296 H H H H CH₃ CH₂CH₂SOCH₃ H H O 0 A-5297 H H H H CH₃ CH₂CH₂CH₂SOCH₃ H H O 0 A-5298 H H H H CH₃ CH(CH₃)SOCH₃ H H O 0 A-5299 H H H H CH₃ CH₂CH(CH₃)SOCH₃ H H O 0 A-5300 H H H H CH₃ CH(CH₃)CH₂CH₂SOCH₃ H H O 0 A-5301 H H H H CH₃ CH₂CH(CH₃)CH₂SOCH₃ H H O 0 A-5302 H H H H CH₃ CH₂CH₂CH(CH₃)SOCH₃ H H O 0

TABLE 88 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5303 H H H H CH₃ CH₂SO₂CH₃ H H O 0 A-5304 H H H H CH₃ CH₂CH₂SO₂CH₃ H H O 0 A-5305 H H H H CH₃ CH₂CH₂CH₂SO₂CH₃ H H O 0 A-5306 H H H H CH₃ CH(CH₃)SO₂CH₃ H H O 0 A-5307 H H H H CH₃ CH₂CH(CH₃)SO₂CH₃ H H O 0 A-5308 H H H H CH₃ CH(CH₃)CH₂CH₂SO₂CH₃ H H O 0 A-5309 H H H H CH₃ CH₂CH(CH₃)CH₂SO₂CH₃ H H O 0 A-5310 H H H H CH₃ CH₂CH₂CH(CH₃)SO₂CH₃ H H O 0 A-5311 H H H H CH₃ CH₂SCF₃ H H O 0 A-5312 H H H H CH₃ CH₂SCHF₂ H H O 0 A-5313 H H H H CH₃ CH₂SCH₂CF₃ H H O 0 A-5314 H H H H CH₃ CH₂SCH₂CHF₂ H H O 0 A-5315 H H H H CH₃ CH₂SCF₂CF₃ H H O 0 A-5316 H H H H CH₃ CH₂CH₂SCF₃ H H O 0 A-5317 H H H H CH₃ CH₂CH₂SCH₂CF₃ H H O 0 A-5318 H H H H CH₃ CH₂CH₂CH₂SCF₃ H H O 0 A-5319 H H H H CH₃ CH₂CH₂CH₂SCH₂CF₃ H H O 0 A-5320 H H H H CH₃ CH(CH₃)SCF₃ H H O 0 A-5321 H H H H CH₃ CH(CH₃)SCH₂CF₃ H H O 0 A-5322 H H H H CH₃ CH₂CH(CH₃)SCF₃ H H O 0 A-5323 H H H H CH₃ CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-5324 H H H H CH₃ CH(CH₃)CH₂CH₂SCF₃ H H O 0 A-5325 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 0 A-5326 H H H H CH₃ CH₂CH(CH₃)CH₂SCF₃ H H O 0 A-5327 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 0 A-5328 H H H H CH₃ CH₂CH₂CH(CH₃)SCF₃ H H O 0 A-5329 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 0 A-5330 H H H H CH₃ CH₂SOCF₃ H H O 0 A-5331 H H H H CH₃ CH₂CH₂SOCF₃ H H O 0 A-5332 H H H H CH₃ CH₂CH₂CH₂SOCF₃ H H O 0 A-5333 H H H H CH₃ CH(CH₃)SOCF₃ H H O 0 A-5334 H H H H CH₃ CH₂CH(CH₃)SOCF₃ H H O 0 A-5335 H H H H CH₃ CH(CH₃)CH₂CH₂SOCF₃ H H O 0 A-5336 H H H H CH₃ CH₂CH(CH₃)CH₂SOCF₃ H H O 0 A-5337 H H H H CH₃ CH₂CH₂CH(CH₃)SOCF₃ H H O 0 A-5338 H H H H CH₃ CH₂SO₂CF₃ H H O 0 A-5339 H H H H CH₃ CH₂CH₂SO₂CF₃ H H O 0 A-5340 H H H H CH₃ CH₂CH₂CH₂SO₂CF₃ H H O 0 A-5341 H H H H CH₃ CH(CH₃)SO₂CF₃ H H O 0 A-5342 H H H H CH₃ CH₂CH(CH₃)SO₂CF₃ H H O 0 A-5343 H H H H CH₃ CH(CH₃)CH₂CH₂SO₂CF₃ H H O 0 A-5344 H H H H CH₃ CH₂CH(CH₃)CH₂SO₂CF₃ H H O 0 A-5345 H H H H CH₃ CH₂CH₂CH(CH₃)SO₂CF₃ H H O 0 A-5346 H H H H CH₃ CH₂C(═O)CH₃ H H O 0 A-5347 H H H H CH₃ CH₂C(═O)CH₂CH₃ H H O 0 A-5348 H H H H CH₃ CH₂C(═O)C(CH₃)₃ H H O 0 A-5349 H H H H CH₃ CH₂CH₂C(═O)CH₃ H H O 0 A-S350 H H H H CH₃ CH₂CH₂C(═O)C(CH₃)₃ H H O 0 A-5351 H H H H CH₃ CH₂C(═O)CF₃ H H O 0 A-5352 H H H H CH₃ CH₂CH₂C(═O)CF₃ H H O 0 A-53S3 H H H H CH₃ CH₂C(═O)OCH₃ H H O 0 A-53S4 H H H H CH₃ CH₂C(═O)OCH₂CH₃ H H O 0 A-5355 H H H H CH₃ CH₂C(═O)OC(CH₃)₃ H H O 0 A-5356 H H H H CH₃ CH₂CH₂C(═O)OCH₃ H H O 0 A-5357 H H H H CH₃ CH₂CH₂C(═O)OCH₂CH₃ H H O 0 A-5358 H H H H CH₃ CH₂CH₂C(═O)OC(CH₃)₃ H H O 0 A-5359 H H H H CH₃ CH₂C(═O)NH₂ H H O 0 A-5360 H H H H CH₃ CH₂CH₂C(═O)NH₂ H H O 0 A-5361 H H H H CH₃ CH₂C(═O)NHCH₃ H H O 0 A-5362 H H H H CH₃ CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-5363 H H H H CH₃ CH₂CH₂C(═O)NHCH₃ H H O 0

TABLE 89 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5364 H H H H CH₃ CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 0 A-5365 H H H H CH₃ CH₂C(═O)NHCH₂CHF₂ H H O 0 A-5366 H H H H CH₃ CH₂C(═O)NHCH₂CF₃ H H O 0 A-5367 H H H H CH₃ CH₂CH₂C(═O)NHCH₂CHF₂ H H O 0 A-5368 H H H H CH₃ CH₂CH₂C(═O)NHCH₂CF₃ H H O 0 A-5369 H H H H CH₃ CH₂C(═O)N(CH₃)₂ H H O 0 A-5370 H H H H CH₃ CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-5371 H H H H CH₃ CH₂CH₂C(═O)N(CH₃)₂ H H O 0 A-5372 H H H H CH₃ CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 0 A-5373 H H H H CH₃ CH₂CH₂OH H H O 0 A-5374 H H H H CH₃ CH₂CH(OH)CH₃ H H O 0 A-5375 H H H H CH₃ CH₂CH₂CH₂OH H H O 0 A-5376 H H H H CH₃ CH₂CH(OH)CH₂CH₃ H H O 0 A-5377 H H H H CH₃ CH₂CH(OH)C(CH₃)₃ H H O 0 A-5378 H H H H CH₃ CH₂CH₂CH(OH)CH₃ H H O 0 A-5379 H H H H CH₃ CH₂CH₂CH(OH)C(CH₃)₃ H H O 0 A-5380 H H H H CH₃ CH₂C(═NOH)CH₃ H H O 0 A-5381 H H H H CH₃ CH₂C(═NOH)CH₂CH₃ H H O 0 A-5382 H H H H CH₃ CH₂C(═NOH)C(CH₃)₃ H H O 0 A-5383 H H H H CH₃ CH₂C(═NOCH₃)CH₃ H H O 0 A-5384 H H H H CH₃ CH₂C(═NOCH₃)CH₂CH₃ H H O 0 A-5385 H H H H CH₃ CH₂C(═NOCH₂CH₃)CH₃ H H O 0 A-5386 H H H H CH₃ CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 0 A-5387 H H H H CH₃ CH₂C(═NOCH₂CF₃)CH₃ H H O 0 A-5388 H H H H CH₃ CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 0 A-5389 H H H H CH₃ CH₂Ph H H O 0 A-5390 H H H H CH₃ CH₂(2-F)Ph H H O 0 A-5391 H H H H CH₃ CH₂(3-F)PH H H O 0 A-5392 H H H H CH₃ CH₂(4-F)Ph H H O 0 A-5393 H H H H CH₃ CH₂(2-Cl)Ph H H O 0 A-5394 H H H H CH₃ CH₂(3-Cl)Ph H H O 0 A-5395 H H H H CH₃ CH₂(4-Cl)Ph H H O 0 A-5396 H H H H CH₃ CH₂(2-CF₃)Ph H H O 0 A-5397 H H H H CH₃ CH₂(3-CF₃)Ph H H O 0 A-5398 H H H H CH₃ CH₂(4-CF₃)Ph H H O 0 A-5399 H H H H CH₃ CH₂(naphthalen-1-yl) H H O 0 A-5400 H H H H CH₃ CH₂(naphthalen-2-yl) H H O 0 A-5401 H H H H CH₃ CH₂CH₂Ph H H O 0 A-5402 H H H H H H H H S 0 A-5403 H H H H H CH₃ H H S 0 A-5404 H H H H H CH₂CH₃ H H S 0 A-5405 H H H H H CH(CH₃)₂ H H S 0 A-5406 H H H H H CH₂CH₂CH₃ H H S 0 A-5407 H H H H H CH₂CH(CH₃)₂ H H S 0 A-5408 H H H H H CH(CH₃)CH₂CH₃ H H S 0 A-5409 H H H H H CH₂C(CH₃)₃ H H S 0 A-5410 H H H H H CH₂(CH₂)₂CH₃ H H S 0 A-5411 H H H H H CH₂(CH₂)₃CH₃ H H S 0 A-5412 H H H H H CF₃ H H S 0 A-5413 H H H H H CHF₂ H H S 0 A-5414 H H H H H CH₂CF₃ H H S 0 A-5415 H H H H H CH₂CHF₂ H H S 0 A-5416 H H H H H CH₂CClF₂ H H S 0 A-5417 H H H H H CH₂CBrF₂ H H S 0 A-5418 H H H H H CF₂CF₃ H H S 0 A-5419 H H H H H CF₂CHF₂ H H S 0 A-5420 H H H H H CH₂CH₂CF₃ H H S 0 A-5421 H H H H H CH₂CF₂CF₃ H H S 0 A-5422 H H H H H CH₂CF₂CHF₂ H H S 0 A-5423 H H H H H CF₂CHFCF₃ H H S 0 A-5424 H H H H H CF₂CF₂CF₃ H H S 0

TABLE 90 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5425 H H H H H CH₂CF₂CF₂CF₃ H H S 0 A-5426 H H H H H CH₂CF₂CHFCF₃ H H S 0 A-5427 H H H H H CH₂CH₂CH₂CF₃ H H S 0 A-5428 H H H H H CH₂CH₂CF₂CF₃ H H S 0 A-5429 H H H H H CF₂CF₂CF₂CF₃ H H S 0 A-5430 H H H H H CH₂CH₂CH(CF₃)₂ H H S 0 A-5431 H H H H H CF₂CF₂CF₂CF₂CF₃ H H S 0 A-5432 H H H H H CH₂CF₂CF₂CF₂CF₃ H H S 0 A-5433 H H H H H CH₂CH₂CH₂CH₂CF₃ H H S 0 A-5434 H H H H H CH₂CF₂CF₂CF₂CHF₂ H H S 0 A-5435 H H H H H CH₂CH₂OCH₂CF₃ H H S 0 A-5436 H H H H H CF₂CHFOCF₃ H H S 0 A-5437 H H H H H CF₂CHFOCF₂CF₃ H H S 0 A-5438 H H H H H CH₂CH₂CF═CF₂ H H S 0 A-5439 H H H H H CH₂CH₂CH═CF₂ H H S 0 A-5440 H H H H H CH₂C═CCH₃ H H S 0 A-5441 H H H H H CH₂C═CCF₃ H H S 0 A-5442 H H H H H CH₂C═CI H H S 0 A-5443 H H H H H CH₂(2,2-difluorocyclopropyl) H H S 0 A-5444 H H H H H CH₂(2,2-dichlorocydopropyl) H H S 0 A-5445 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) H H S 0 A-5446 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H H S 0 A-5447 H H H H H CH₂SCH₃ H H S 0 A-5448 H H H H H CH₂SCH₂CH₃ H H S 0 A-5449 H H H H H CH₂CH₂SCH₃ H H S 0 A-5450 H H H H H CH₂SOCH₃ H H S 0 A-5451 H H H H H CH₂CH₂SOCH₃ H H S 0 A-5452 H H H H H CH₂SO₂CH₃ H H S 0 A-5453 H H H H H CH₂CH₂SO₂CH₃ H H S 0 A-5454 H H H H H CH₂SCF₃ H H S 0 A-5455 H H H H H CH₂SCHF₂ H H S 0 A-5456 H H H H H CH₂SCH₂CF₃ H H S 0 A-5457 H H H H H CH₂SCH₂CHF₂ H H S 0 A-5458 H H H H H CH₂SCF₂CF₃ H H S 0 A-5459 H H H H H CH₂CH₂SCF₃ H H S 0 A-5460 H H H H H CH₂SOCF₃ H H S 0 A-5461 H H H H H CH₂CH₂SOCF₃ H H S 0 A-5462 H H H H H CH₂CH₂CH₂SOCF₃ H H S 0 A-5463 H H H H H CH₂SO₂CF₃ H H S 0 A-5464 H H H H H CH₂CH₂SO₂CF₃ H H S 0 A-5465 H H H H H CH₂CH₂CH₂SO₂CF₃ H H S 0 A-5466 H H H H H CH₂C(═O)NHCH₂CHF₂ H H S 0 A-5467 H H H H H CH₂C(═O)NHCH₂CF₃ H H S 0 A-546 8 H H H H H H H H O 1 A-5469 H H H H H CH₃ H H O 1 A-5470 H H H H H CH₂CH₃ H H O 1 A-5471 H H H H H CH(CH₃)₂ H H O 1 A-5472 H H H H H CH₂CH₂CH₃ H H O 1 A-5473 H H H H H CH₂CH(CH₃)₂ H H O 1 A-5474 H H H H H CH(CH₃)CH₂CH₃ H H O 1 A-5475 H H H H H CH₂C(CH₃)₃ H H O 1 A-5476 H H H H H CH₂(CH₂)₂CH₃ H H O 1 A-5477 H H H H H CH₂(CH₂)₃CH₃ H H O 1 A-5478 H H H H H CH₂(CH₂)₄CH₃ H H O 1 A-5479 H H H H H CH₂(CH₂)₆CH₃ H H O 1 A-5480 H H H H H CH₂OCH₃ H H O 1 A-5481 H H H H H CH₂OCH₂CH₃ H H O 1 A-5482 H H H H H CH₂CH₂OCH₃ H H O 1 A-5483 H H H H H CH₂CH₂OCH₂CH₃ H H O 1 A-5484 H H H H H CF₃ H H O 1 A-5485 H H H H H CHF₂ H H O 1

TABLE 91 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5486 H H H H H CH₂CF₃ H H O 1 A-5487 H H H H H CH₂CHF₂ H H O 1 A-5488 H H H H H CH₂CClF₂ H H O 1 A-5489 H H H H H CH₂CBrF₂ H H O 1 A-5490 H H H H H CF₂CF₃ H H O 1 A-5491 H H H H H CF₂CHF₂ H H O 1 A-5492 H H H H H CH₂CH₂CF₃ H H O 1 A-5493 H H H H H CH₂CF₂CF₃ H H O 1 A-5494 H H H H H CH₂CF₂CHF₂ H H O 1 A-5495 H H H H H CF₂CHFCF₃ H H O 1 A-5496 H H H H H CF₂CF₂CF₃ H H O 1 A-5497 H H H H H CH₂CF₂CF₂CF₃ H H O 1 A-5498 H H H H H CH₂CH₂CH₂CF₃ H H O 1 A-5499 H H H H H CH₂CH₂CF₂CF₃ H H O 1 A-5500 H H H H H CF₂CF₂CF₂CF₃ H H O 1 A-5501 H H H H H CH₂CH₂CH(CF₃)₂ H H O 1 A-5502 H H H H H CF₂CF₂CF₂CF₂CF₃ H H O 1 A-5503 H H H H H CH₂CF₂CF₂CF₂CF₃ H H O 1 A-5504 H H H H H CH₂CH₂CH₂CH₂CF₃ H H O 1 A-5505 H H H H H CH₂CF₂CF₂CF₂CHF₂ H H O 1 A-5506 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H H O 1 A-5507 H H H H H CF₂CHFOCH₃ H H O 1 A-5508 H H H H H CF₂CHFOCH₂CH₃ H H O 1 A-5509 H H H H H CH₂CH₂OCH₂CF₃ H H O 1 A-5510 H H H H H CF₂CHFOCF₃ H H O 1 A-5511 H H H H H CF₂CHFOCF₂CF₃ H H O 1 A-5512 H H H H H CF₂CHFOCF₂CF₂CF₃ H H O 1 A-5513 H H H H H CH₂CH═CH₂ H H O 1 A-5514 H H H H H CH₂CH═CHCl H H O 1 A-5515 H H H H H CH₂CH═CCl₂ H H O 1 A-5516 H H H H H CH₂CH₂CF═CF₂ H H O 1 A-5517 H H H H H CH₂CH₂CH═CF₂ H H O 1 A-5518 H H H H H CH₂C═CH H H O 1 A-5519 H H H H H CH₂C═CCH₃ H H O 1 A-5520 H H H H H CH₂C═CCF₃ H H O 1 A-5521 H H H H H CH₂C═CI H H O 1 A-5522 H H H H H cyclobutyl H H O 1 A-5523 H H H H H cyclopentyl H H O 1 A-5524 H H H H H cyclohexyl H H O 1 A-5525 H H H H H 4,4-difluorocyclohexyl H H O 1 A-5526 H H H H H CH₂(cyclopropyl) H H O 1 A-5527 H H H H H CH₂(cyclobutyl) H H O 1 A-5528 H H H H H CH₂(cyclopentyl) H H O 1 A-5529 H H H H H CH₂CH₂(cyclopropyl) H H O 1 A-5530 H H H H H CH₂(2,2-difluorocyclopropyl) H H O 1 A-5531 H H H H H CH₂(2,2-dichlorocyclopropyl) H H O 1 A-5532 H H H H H CH₂(4,4-difluorocyclohexyl) H H O 1 A-5533 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) H H O 1 A-5534 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H H O 1 A-5535 H H H H H CH₂SCH₃ H H O 1 A-5536 H H H H H CH₂SCH₂CH₃ H H O 1 A-5537 H H H H H CH₂CH₂SCH₃ H H O 1 A-5538 H H H H H CH₂CH₂SCH₂CH₃ H H O 1 A-5539 H H H H H CH₂CH₂CH₂SCH₃ H H O 1 A-5540 H H H H H CH₂CH₂CH₂SCH₂CH₃ H H O 1 A-5541 H H H H H CH(CH₃)SCH₃ H H O 1 A-5542 H H H H H CH(CH₃)SCH₂CH₃ H H O 1 A-5543 H H H H H CH₂CH(CH₃)SCH₃ H H O 1 A-5544 H H H H H CH₂CH(CH₃)SCH₂CH₃ H H O 1 A-5545 H H H H H CH(CH₃)CH₂CH₂SCH₃ H H O 1 A-5546 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H H O 1

TABLE 92 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5547 H H H H H CH₂CH(CH₃)CH₂SCH₃ H H O 1 A-5548 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H H O 1 A-5549 H H H H H CH₂CH₂CH(CH₃)SCH₃ H H O 1 A-5550 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H H O 1 A-5551 H H H H H CH₂SOCH₃ H H O 1 A-5552 H H H H H CH₂CH₂SOCH₃ H H O 1 A-5553 H H H H H CH₂CH₂CH₂SOCH₃ H H O 1 A-5554 H H H H H CH(CH₃)SOCH₃ H H O 1 A-5555 H H H H H CH₂CH(CH₃)SOCH₃ H H O 1 A-5556 H H H H H CH(CH₃)CH₂CH₂SOCH₃ H H O 1 A-5557 H H H H H CH₂CH(CH₃)CH₂SOCH₃ H H O 1 A-5558 H H H H H CH₂CH₂CH(CH₃)SOCH₃ H H O 1 A-5559 H H H H H CH₂SO₂CH₃ H H O 1 A-5560 H H H H H CH₂CH₂SO₂CH₃ H H O 1 A-5561 H H H H H CH₂CH₂CH₂SO₂CH₃ H H O 1 A-5562 H H H H H CH(CH₃)SO₂CH₃ H H O 1 A-5563 H H H H H CH₂CH(CH₃)SO₂CH₃ H H O 1 A-5564 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ H H O 1 A-5565 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ H H O 1 A-5566 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ H H O 1 A-5567 H H H H H CH₂SCF₃ H H O 1 A-5568 H H H H H CH₂SCHF₂ H H O 1 A-5569 H H H H H CH₂SCH₂CF₃ H H O 1 A-5570 H H H H H CH₂SCH₂CHF₂ H H O 1 A-5571 H H H H H CH₂SCF₂CF₃ H H O 1 A-5572 H H H H H CH₂CH₂SCF₃ H H O 1 A-5573 H H H H H CH₂CH₂SCH₂CF₃ H H O 1 A-5574 H H H H H CH₂CH₂CH₂SCF₃ H H O 1 A-5575 H H H H H CH₂CH₂CH₂SCH₂CF₃ H H O 1 A-5576 H H H H H CH(CH₃)SCF₃ H H O 1 A-5577 H H H H H CH(CH₃)SCH₂CF₃ H H O 1 A-5578 H H H H H CH₂CH(CH₃)SCF₃ H H O 1 A-5579 H H H H H CH₂CH(CH₃)SCH₂CF₃ H H O 1 A-5580 H H H H H CH(CH₃)CH₂CH₂SCF₃ H H O 1 A-5581 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H H O 1 A-5582 H H H H H CH₂CH(CH₃)CH₂SCF₃ H H O 1 A-5583 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H H O 1 A-5584 H H H H H CH₂CH₂CH(CH₃)SCF₃ H H O 1 A-5585 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H H O 1 A-5586 H H H H H CH₂SOCF₃ H H O 1 A-5587 H H H H H CH₂CH₂SOCF₃ H H O 1 A-5588 H H H H H CH₂CH₂CH₂SOCF₃ H H O 1 A-5589 H H H H H CH(CH₃)SOCF₃ H H O 1 A-5590 H H H H H CH₂CH(CH₃)SOCF₃ H H O 1 A-S591 H H H H H CH(CH₃)CH₂CH₂SOCF₃ H H O 1 A-5592 H H H H H CH₂CH(CH₃)CH₂SOCF₃ H H O 1 A-5593 H H H H H CH₂CH₂CH(CH₃)SOCF₃ H H O 1 A-5594 H H H H H CH₂SO₂CF₃ H H O 1 A-5595 H H H H H CH₂CH₂SO₂CF₃ H H O 1 A-5596 H H H H H CH₂CH₂CH₂SO₂CF₃ H H O 1 A-5597 H H H H H CH(CH₃)SO₂CF₃ H H O 1 A-5598 H H H H H CH₂CH(CH₃)SO₂CF₃ H H O 1 A-5599 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ H H O 1 A-5600 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ H H O 1 A-5601 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ H H O 1 A-5602 H H H H H CH₂C(═O)CH₃ H H O 1 A-5603 H H H H H CH₂C(═O)CH₂CH₃ H H O 1 A-5604 H H H H H CH₂C(═O)C(CH₃)₃ H H O 1 A-5605 H H H H H CH₂CH₂C(═O)CH₃ H H O 1 A-5606 H H H H H CH₂CH₂C(═O)C(CH₃)₃ H H O 1 A-5607 H H H H H CH₂C(═O)CF₃ H H O 1

TABLE 93 Compound R¹ R² R³ R⁴ R⁵ R⁶ R⁷ R⁸ X n A-5608 H H H H H CH₂CH₂C(═O)CF₃ H H O 1 A-5609 H H H H H CH₂C(═O)OCH₃ H H O 1 A-5610 H H H H H CH₂C(═O)OCH₂CH₃ H H O 1 A-5611 H H H H H CH₂C(═O)OC(CH₃)₃ H H O 1 A-5612 H H H H H CH₂CH₂C(═O)OCH₃ H H O 1 A-5613 H H H H H CH₂CH₂C(═O)OCH₂CH₃ H H O 1 A-5614 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ H H O 1 A-5615 H H H H H CH₂C(═O)NH₂ H H O 1 A-5616 H H H H H CH₂CH₂C(═O)NH₂ H H O 1 A-5617 H H H H H CH₂C(═O)NHCH₃ H H O 1 A-5618 H H H H H CH₂C(═O)NHCH(CH₂)₂ H H O 1 A-5619 H H H H H CH₂CH₂C(═O)NHCH₃ H H O 1 A-5620 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ H H O 1 A-5621 H H H H H CH₂C(═O)NHCH₂CHF₂ H H O 1 A-5622 H H H H H CH₂C(═O)NHCH₂CF₃ H H O 1 A-5623 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ H H O 1 A-5624 H H H H H CH₂CH₂C(═ O)NHCH₂CF₃ H H O 1 A-5625 H H H H H CH₂C(═O)N(CH₃)₂ H H O 1 A-5626 H H H H H CH₂C(═O)N(CH₂CH₃)₂ H H O 1 A-5627 H H H H H CH₂CH₂C(═O)N(CH₃)₂ H H O 1 A-5628 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H H O 1 A-5629 H H H H H CH₂CH₂OH H H O 1 A-5630 H H H H H CH₂CH(OH)CH₃ H H O 1 A-5631 H H H H H CH₂CH₂CH₂OH H H O 1 A-5632 H H H H H CH₂CH(OH)CH₂CH₃ H H O 1 A-5633 H H H H H CH₂CH(OH)C(CH₃)₃ H H O 1 A-5634 H H H H H CH₂CH₂CH(OH)CH₃ H H O 1 A-5635 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ H H O 1 A-5636 H H H H H CH₂C(═NOH)CH₃ H H O 1 A-5637 H H H H H CH₂C(═NOH)CH₂CH₃ H H O 1 A-5638 H H H H H CH₂C(═NOH)C(CH₃)₃ H H O 1 A-5639 H H H H H CH₂C(═NOCH₃)CH₃ H H O 1 A-5640 H H H H H CH₂C(═NOCH₃)CH₂CH₃ H H O 1 A-5641 H H H H H CH₂C(═NOCH₂CH₃)CH₃ H H O 1 A-5642 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H H O 1 A-5643 H H H H H CH₂C(═NOCH₂CF₃)CH₃ H H O 1 A-5644 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H H O 1 A-5645 H H H H H CH₂Ph H H O 1 A-5646 H H H H H CH₂(2-F)Ph H H O 1 A-5647 H H H H H CH₂(3-F)Ph H H O 1 A-5648 H H H H H CH₂(4-F)Ph H H O 1 A-5649 H H H H H CH₂(2-Cl)Ph H H O 1 A-5650 H H H H H CH₂(3-Cl)Ph H H O 1 A-5651 H H H H H CH₂(4-Cl)Ph H H O 1 A-5652 H H H H H CH₂(2-CF₃)Ph H H O 1 A-5653 H H H H H CH₂(3-CF₃)Ph H H O 1 A-5654 H H H H H CH₂(4-CF₃)Ph H H O 1 A-5655 H H H H H CH₂(naphthalen-1-yl) H H O 1 A-5656 H H H H H CH₂(naphthalen-2-yl) H H O 1 A-5657 H H H H H CH₂CH₂Ph H H O 1 A-5658 H H H H H CH₂CH₂CF₂CF₂CF₂CF₃ H H O 0

TABLE 94

Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0001 H H H H H H H 0 B-0002 H H H H H CH₃ H 0 B-0003 H H H H H CH₂CH₃ H 0 B-0004 H H H H H CH(CH₃)₂ H 0 B-0005 H H H H H C(CH₃)₃ H 0 B-0006 H H H H H CH₂CH₂CH₃ H 0 B-0007 H H H H H CH₂CH(CH₃)₂ H 0 B-0008 H H H H H CH(CH₃)CH₂CH₃ H 0 B-0009 H H H H H CH(CH₂CH₃)CH₂CH₃ H 0 B-0010 H H H H H CH₂C(CH₃)₃ H 0 B-0011 H H H H H CH₂(CH₂)₂CH₃ H 0 B-0012 H H H H H CH₂CH₂CH(CH₃)₂ H 0 B-0013 H H H H H CH₂CH(CH₃)CH₂CH₃ H 0 B-0014 H H H H H CH(CH₃)CH₂CH₂CH₃ H 0 B-0015 H H H H H CH₂CH(CH₂CH₃)CH₂CH₃ H 0 B-0016 H H H H H CH(CH₂CH₃)CH₂CH₂CH₃ H 0 B-0017 H H H H H CH₂CH₂C(CH₃)₃ H 0 B-0018 H H H H H CH₂(CH₂)₃CH₃ H 0 B-0019 H H H H H CH₂CH₂CH₂CH(CH₃)₂ H 0 B-0020 H H H H H CH₂(CH₂)₄CH₃ H 0 B-0021 H H H H H CH₂CH₂CH₂CH₂CH(CH₃)₂ H 0 B-0022 H H H H H CH₂(CH₂)₅CH₃ H 0 B-0023 H H H H H CH₂(CH₂)₆CH₃ H 0 B-0024 H H H H H CH₂OCH₃ H 0 B-0025 H H H H H CH₂OCH₂CH₃ H 0 B-0026 H H H H H CH₂CH₂OCH₃ H 0 B-0027 H H H H H CH₂CH₂OCH₂CH₃ H 0 B-0028 H H H H H CH₂CH₂CH₂OCH₃ H 0 B-0029 H H H H H CH₂CH₂CH₂OCH₂CH₃ H 0 B-0030 H H H H H CF₃ H 0 B-0031 H H H H H CHF₂ H 0 B-0032 H H H H H CH₂CF₃ H 0 B-0033 H H H H H CH₂CHF₂ H 0 B-0034 H H H H H CH₂CClF₂ H 0 B-0035 H H H H H CF₂CHCl₂ H 0 B-0036 H H H H H CF₂CCl₃ H 0 B-0037 H H H H H CH₂CH₂Cl H 0 B-0038 H H H H H CHClCHCl₂ H 0 B-0039 H H H H H CH₂CCl₃ H 0 B-0040 H H H H H CH₂CBrF₂ H 0 B-0041 H H H H H CF₂CF₃ H 0 B-0042 H H H H H CF₂CHF₂ H 0 B-0043 H H H H H CH₂CH₂CF₃ H 0 B-0044 H H H H H CH₂CF₂CF₃ H 0 B-0045 H H H H H CH₂CF₂CHF₂ H 0 B-0046 H H H H H CF₂CHFCF₃ H 0 B-0047 H H H H H CF₂CF₂CF₃ H 0 B-0048 H H H H H CH₂CH₂CH₂Cl H 0 B-0049 H H H H H CH₂CHClCH₂Cl H 0 B-0050 H H H H H CH₂CF₂CF₂CF₃ H 0 B-0051 H H H H H CH₂CF₂CHFCF₃ H 0 B-0052 H H H H H CH₂CH₂CH₂CF₃ H 0 B-0053 H H H H H CH₂CH₂CF₂CF₃ H 0 B-0054 H H H H H CF₂CF₂CF₂CF₃ H 0 B-0055 H H H H H CH₂CH₂CH(CF₃)₂ H 0 B-0056 H H H H H CH₂CH₂CH(CH₃)CF₃ H 0

TABLE 95 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0057 H H H H H CF₂CF₂CF₂CF₂CF₃ H 0 B-0058 H H H H H CH₂CF₂CF₂CF₂CF₃ H 0 B-0059 H H H H H CH₂CH₂CH₂CH₂CF₃ H 0 B-0060 H H H H H CH₂CF₂CF₂CF₂CHF₂ H 0 B-0061 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-0062 H H H H H CH₂CF₂CF₂CF₂CF₂CF₃ H 0 B-0063 H H H H H CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-0064 H H H H H CH₂CF₂CF₂CF₂CF₂CHF₂ H 0 B-0065 H H H H H CH₂CF₂CF₂CF₂CF₂CF₂CF₃ H 0 B-0066 H H H H H CH₂CH₂CH₂CH₂CH_(;)CH₂CF₃ H 0 B-0057 H H H H H CH₂CF₂CF₂CF₂CF₂CF₂CHF₂ H 0 B-0068 H H H H H CF₂CHFOCH₃ H 0 B-0069 H H H H H CF₂CHFOCH₂CH₃ H 0 B-0070 H H H H H CH₂CH₂OCH₂CF₃ H 0 B-0071 H H H H H CF₂CHFOCF₃ H 0 B-0072 H H H H H CF₂CHFOCF₂CF₃ H 0 B-0073 H H H H H CF₂CHFOCF₂CF₂CF₃ H 0 B-0074 H H H H H CH₂CH═CH₂ H 0 B-0075 H H H H H CH₂CH═CHCl H 0 B-0076 H H H H H CH₂CH═CCl₂ H 0 B-0077 H H H H H CH₂CH═C(CH₃)CF₃ H 0 B-0078 H H H H H CH₂CH₃CF═CF₂ H 0 B-0079 H H H H H CH₂CH₂CH═CF₂ H 0 B-0080 H H H H H CH₂C≡CH H 0 B-0081 H H H H H CH₂C≡CCH₃ H 0 B-0082 H H H H H CH₂C≡SCC(CH₃)₃ H 0 B-0083 H H H H H CH₂C≡SC(cyclopropyl) H 0 B-0084 H H H H H CH₂C≡CI H 0 B-0085 H H H H H CH₂C≡CCF₃ H 0 B-0086 H H H H H cyclopropyl H 0 B-0087 H H H H H cyclobutyl H 0 B-0088 H H H H H cyclopentyl H 0 B-0089 H H H H H cyclohexyl H 0 B-0090 H H H H H 4,4-difluorocyclohexyl H 0 B-0091 H H H H H 4-trifluoromethylcyclohexyl H 0 B-0092 H H H H H CH₂(cyclopropyl) H 0 B-0093 H H H H H CH₂(cyclobutyl) H 0 B-0094 H H H H H CH₂(cyclopentyl) H 0 B-0095 H H H H H CH₂(cyclohexyl) H 0 B-0096 H H H H H CH₂CH₂(cyclopropyl) H 0 B-0097 H H H H H CH₂(2,2-difluorocyclopropyl) H 0 B-0098 H H H H H CH₂(2,2-dichlorocyclopropyl) H 0 B-0099 H H H H H CH₂(4,4-difluorocyclohexyl) H 0 B-0100 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-0101 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-0102 H H H H H CH₂CH₂(4,4-difluorocyclohexyl) H 0 B-0103 H H H H H CH₂SCH₃ H 0 B-0104 H H H H H CH₂SCH₂CH₃ H 0 B-0105 H H H H H CH₂CH₂SCH₃ H 0 B-0106 H H H H H CH₂CH₂SCH₂CH₃ H 0 B-0107 H H H H H CH₂CH₂CH₂SCH₃ H 0 B-0108 H H H H H CH₂CH₂CH₂SCH₂CH₃ H 0 B-0109 H H H H H CH(CH₃)SCH₃ H 0 B-0110 H H H H H CH(CH₃)SCH₂CH₃ H 0 B-0111 H H H H H CH₂CH(CH₃)SCH₃ H 0 B-0112 H H H H H CH₂CH(CH₃)SCH₂CH₃ H 0 B-0113 H H H H H CH₂CH₂SCH(CH₃)₂ H 0 B-0114 H H H H H CH(CH₃)CH₂CH₂SCH₃ H 0 B-0115 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-0116 H H H H H CH₂CH(CH₃)CH₂SCH₃ H 0 B-0117 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H 0

TABLE 96 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0118 H H H H H CH₂CH₂CH(CH₃)SCH₃ H 0 B-0119 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-0120 H H H H H CH₂CH₂CH₂CH₂SCH₃ H 0 B-0121 H H H H H CH₂CH₂CH₂CH₂CH₂SCH₃ H 0 B-0122 H H H H H CH₂SOCH₃ H 0 B-0123 H H H H H CH₂CH₂SOCH₃ H 0 B-0124 H H H H H CH₂CH₂SOCH₂CH₃ H 0 B-0125 H H H H H CH₂CH₂SOCH(CH₃)₂ H 0 B-0126 H H H H H CH₂CH₂CH₂SOCH₃ H 0 B-0127 H H H H H CH(CH₃)SOCH₃ H 0 B-0128 H H H H H CH₂CH(CH₃)SOCH₃ H 0 B-0129 H H H H H CH(CH₃)CH₂CH₂SOCH₃ H 0 B-0130 H H H H H CH₂CH(CH₃)CH₂SOCH₃ H 0 B-0131 H H H H H CH₂CH₂CH(CH₃)SOCH₃ H 0 B-0132 H H H H H CH₂CH₂CH₂CH₂SOCH₃ H 0 B-0133 H H H H H CH₂CH₂CH₂CH₂CH₂SOCH₃ H 0 B-0134 H H H H H CH₂SO₂CH₃ H 0 B-0135 H H H H H CH₂CH₂SO₂CH₃ H 0 B-0136 H H H H H CH₂CH₂SO₂CH₂CH₃ H 0 B-0137 H H H H H CH₂CH₂SO₂CH(CH₃)₂ H 0 B-0138 H H H H H CH₂CH₂CH₂SO₂CH₃ H 0 B-0139 H H H H H CH(CH₃)SO₂CH₃ H 0 B-0140 H H H H H CH₂CH(CH₃)SO₂CH₃ H 0 B-0141 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-0142 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-0143 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-0144 H H H H H CH₂CH₂CH₃CH₂SO₂CH₃ H 0 B-0145 H H H H H CH₂CH₂CH₂CH₂CH₂SO₂CH₃ H 0 B-0146 H H H H H CH₂SCF₃ H 0 B-0147 H H H H H CH₂SCHF₂ H 0 B-0148 H H H H H CH₂SCH₂CF₃ H 0 B-0149 H H H H H CH₂SCH₂CHF₂ H 0 B-0150 H H H H H CH₂SCF₂CF₃ H 0 B-0151 H H H H H CH₂CH₂SCF₃ H 0 B-0152 H H H H H CH₂CH₂SCH₂CF₃ H 0 B-0153 H H H H H CH₂CH₂CH₂SCF₃ H 0 B-0154 H H H H H CH₂CH₂CH₂SCH₂CF₃ H 0 B-0155 H H H H H CH(CH₃)SCF₃ H 0 B-0156 H H H H H CH(CH₃)SCH₂CF₃ H 0 B-0157 H H H H H CH₂CH(CH₃)SCF₃ H 0 B-0158 H H H H H CH₂CH(CH₃)SCH₂CF₃ H 0 B-0159 H H H H H CH(CH₃)CH₂CH₂SCF₃ H 0 B-0160 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-0161 H H H H H CH₂CH(CH₃)CH₂SCF₃ H 0 B-0162 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-0163 H H H H H CH₂CH₂CH(CH₃)SCF₃ H 0 B-0164 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-0165 H H H H H CH₂CH₂CH₂CH₃SCF₃ H 0 B-0166 H H H H H CH₂CH₂CH₂CH₂CH₂SCF₃ H 0 B-0167 H H H H H CH₂SOCF₃ H 0 B-0168 H H H H H CH₂CH₂SOCF₃ H 0 B-0169 H H H H H CH₂CH₂CH₂SOCF₃ H 0 B-0170 H H H H H CH(CH₃)SOCF₃ H 0 B-0171 H H H H H CH₂CH(CH₃)SOCF₃ H 0 B-0172 H H H H H CH(CH₃)CH₂CH₂SOCF₃ H 0 B-0173 H H H H H CH₂CH(CH₃)CH₂SOCF₃ H 0 B-0174 H H H H H CH₂CH₂CH(CH₃)SOCF_(S) H 0 B-0175 H H H H H CH₂SO₂CF₃ H 0 B-0176 H H H H H CH₂CH₂SO₃CF₃ H 0 B-0177 H H H H H CH₂CH₂SO₂CH₂CF₃ H 0 B-0178 H H H H H CH₂CH₂CH₂SO₂CF₃ H 0

TABLE 97 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0179 H H H H H CH(CH₃)SO₂CF₃ H 0 B-0180 H H H H H CH₂CH(CH₃)SO₂CF₃ H 0 B-0181 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-0182 H H H H H CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-0183 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-0184 H H H H H CH₂C(═O)CH₃ H 0 B-0185 H H H H H CH₂C(═O)CH₂CH₃ H 0 B-0186 H H H H H CH₂C(═O)C(CH₃)₃ H 0 B-0187 H H H H H CH₂CF₂C(═O)CH₃ H 0 B-0188 H H H H H CH₂CH₂C(═O)C(CH₃)₃ H 0 B-0189 H H H H H CH₂C(═O)CF₃ H 0 B-0190 H H H H H CH₂CH₂C(═O)CF₃ H 0 B-0191 H H H H H CH₂C(═O)OCH₃ H 0 B-0192 H H H H H CH₂C(═O)OCH₂CH₂ H 0 B-0193 H H H H H CH₂C(═O)OC(CH₃)₃ H 0 B-0194 H H H H H CH₂CH₂C(═O)OCH₃ H 0 B-0195 H H H H H CH₂CH₂C(═O)OCH₂CH₃ H 0 B-0196 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-0197 H H H H H CH₂C(═O)NH₂ H 0 B-0198 H H H H H CH₂CH₂C(═O)NH₂ H 0 B-0199 H H H H H CH₂C(═O)NHCH₃ H 0 B-0200 H H H H H CH₂C(═O)NHCH(CH₃)₂ H 0 B-0201 H H H H H CH₂CH₂C(═O)NHCH₃ H 0 B-0202 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-0203 H H H H H CH₂C(═O)NH(cyclopropyl) H 0 B-0204 H H H H H CH₂C(═O)NHCH₂CHF₂ H 0 B-0205 H H H H H CH₂C(═O)NHCH₂CF₃ H 0 B-0206 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ H 0 B-0207 H H H H H CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-0208 H H H H H CH(CH₃)C(═O)NHCH₂CHF₂ H 0 B-0209 H H H H H CH(CH₃)C(═O)NHCH₂CF₃ H 0 B-0210 H H H H H C(CH₃)₂C(═O)NHCH₂CHF₂ H 0 B-0211 H H H H H C(CH₃)₂C(═O)NHCH₂CF₃ H 0 B-0212 H H H H H CH₂C(═O)N(CH₃)₂ H 0 B-0213 H H H H H CH₂C(═O)N(CH₂CH₃)₂ H 0 B-0214 H H H H H CH₂CH₂C(═O)N(CH₃)₂ H 0 B-0215 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-0216 H H H H H CH₂CH₂NHC(═O)OCH₃ H 0 B-0217 H H H H H CH₂CH₂NHC(═O)OC(CH₃)₃ H 0 B-0218 H H H H H CH₂CH₂CH₂NHC(═O)OCH₃ H 0 B-0219 H H H H H CH₂CH₂CH₂NHC(═O)OC(CH₃)₃ H 0 B-0220 H H H H H CH₂CH₂NHSO₂CHF₂ H 0 B-0221 H H H H H CH₂CH₂NHSO₂CF₃ H 0 B-0222 H H H H H CH₂CH₂CH₂NHSO₂CHF₂ H 0 B-0223 H H H H H CH₂CH₂CH₂NHSO₂CF₃ H 0 B-0224 H H H H H CH₂CH₂OH H 0 B-0225 H H H H H CH₂CH(OH)CH₃ H 0 B-0226 H H H H H CH₂CH₂CH₂OH H 0 B-0227 H H H H H CH₂CH(OH)CH₂CH₃ H 0 B-0228 H H H H H CH₂CH(OH)C(CH₃)₃ H 0 B-0229 H H H H H CH₂CH₂CH(OH)CH₃ H 0 B-0230 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-0231 H H H H H CH₂C(═NOH)CH₃ H 0 B-0232 H H H H H CH₂C(═NOH)CH₂CH₃ H 0 B-0233 H H H H H CH₂C(═NOH)C(CH₃)₃ H 0 B-0234 H H H H H CH₂C(═NOCH₃)CH₃ H 0 B-0235 H H H H H CH₂C(═NOCH₃)CH₂CH₃ H 0 B-0236 H H H H H CH₂C(═NOCH₂CH₃)CH₃ H 0 B-0237 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-0238 H H H H H CH₂C(═NOCH₂CF₃)CH₃ H 0 B-0239 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0

TABLE 98 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0240 H H H H H CH₂Ph H 0 B-0241 H H H H H CH₂(2-F)Ph H 0 B-0242 H H H H H CH₂(3-F)Ph H 0 B-0243 H H H H H CH₂(4-F)Ph H 0 B-0244 H H H H H CH₂(2-Cl)Ph H 0 B-0245 H H H H H CH₂(3-Cl)Ph H 0 B-0246 H H H H H CH₂(4-Cl)Ph H 0 B-0247 H H H H H CH₂(2-CF₃)Ph H 0 B-0248 H H H H H CH₂(3-CF₃)Ph H 0 B-0249 H H H H H CH₂(4-CF₃)Ph H 0 B-0250 H H H H H CH₂(2-F-4-CF₃)Ph H 0 B-0251 H H H H H CH₂(napnthalen-1-yl) H 0 B-0252 H H H H H CH₂(naphthalen-2-yl) H 0 B-0253 H H H H H CH(CH₃)Ph H 0 B-0254 H H H H H CH₂CH₂Ph H 0 B-0255 H H H H H H CH₂CH₃ 0 B-0256 H H H H H CH₃ CH₂CH₃ 0 B-0257 H H H H H CH₂CH₃ CH₂CH₃ 0 B-0258 H H H H H CH(CH₃)₂ CH₂CH₃ 0 B-0259 H H H H H C(CH₃)₃ CH₂CH₃ 0 B-0260 H H H H H CH₂CH₂CH₃ CH₂CH₃ 0 B-0261 H H H H H CH₂CH(CH₃)₂ CH₂CH₃ 0 B-0262 H H H H H CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-0263 H H H H H CH(CH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-0264 H H H H H CH₂C(CH₃)₃ CH₂CH₃ 0 B-0265 H H H H H CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-0266 H H H H H CH₂CH₂CH(CH₃)₂ CH₂CH₃ 0 B-0267 H H H H H CH₂CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-0268 H H H H H CH(CH₃)CH₂CH₂CH₃ CH₂CH₃ 0 B-0269 H H H H H CH₂CH(CH₂CH₃)CH₃CH₃ CH₂CH₃ 0 B-0270 H H H H H CH(CH₂CH₃)CH₂CH₂CH₃ CH₂CH₃ 0 B-0271 H H H H H CH₂CH₂C(CH₃)₃ CH₂CH₃ 0 B-0272 H H H H H CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-0273 H H H H H CH₂CH₂CH₂CH(CH₃)₃ CH₂CH₃ 0 B-0274 H H H H H CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-0275 H H H H H CH₂CH₂CH₂CH₂CH(CH₃)₂ CH₂CH₃ 0 B-0276 H H H H H CH₂(CH₂)₅CH₃ CH₂CH₃ 0 B-0277 H H H H H CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-0278 H H H H H CH₂OCH₃ CH₂CH₃ 0 B-0279 H H H H H CH₂OCH₂CH₃ CH₂CH₃ 0 B-0280 H H H H H CH₂CH₂OCH₃ CH₂CH₃ 0 B-0281 H H H H H CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-0282 H H H H H CH₂CH₂CH₂OCH₃ CH₂CH₃ 0 B-0283 H H H H H CH₂CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-0284 H H H H H CF₃ CH₂CH₃ 0 B-0285 H H H H H CHF₂ CH₂CH₃ 0 B-0286 H H H H H CH₂CF₃ CH₃CH₃ 0 B-0287 H H H H H CH₂CHF₂ CH₂CH₃ 0 B-0288 H H H H H CH₂CClF₂ CH₂CH₃ 0 B-0289 H H H H H CF₂CHCl₂ CH₂CH₃ 0 B-0290 H H H H H CF₂CCl₃ CH₂CH₃ 0 B-0291 H H H H H CH₂CH₂Cl CH₂CH₃ 0 B-0292 H H H H H CHClCHCl₂ CH₂CH₃ 0 B-0293 H H H H H CH₂CCl₃ CH₂CH₃ 0 B-0294 H H H H H CH₂CBrF₂ CH₂CH₃ 0 B-0295 H H H H H CF₂CF₃ CH₂CH₃ 0 B-0296 H H H H H CF₂CHF₂ CH₂CH₃ 0 B-0297 H H H H H CH₂CH₂CF₃ CH₂CH₃ 0 B-0298 H H H H H CH₂CF₂CF₃ CH₂CH₃ 0 B-0299 H H H H H CH₂CF₂CHF₂ CH₂CH₃ 0 B-0300 H H H H H CF₂CHFCF₃ CH₂CH₃ 0

TABLE 99 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0301 H H H H H CF₂CF₂CF₃ CH₂CH₃ 0 B-0302 H H H H H CH₂CH₂CH₂Cl CH₂CH₃ 0 B-0303 H H H H H CH₂CHClCH₂Cl CH₂CH₃ 0 B-0304 H H H H H CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0305 H H H H H CH₂CF₂CHFCF₃ CH₂CH₃ 0 B-0306 H H H H H CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0307 H H H H H CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-0308 H H H H H CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0309 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-0310 H H H H H CH₂CH₂CH(CH₃)CF₃ CH₂CH₃ 0 B-0311 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0312 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0313 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0314 H H H H H CH₂CF₂CF₂CF₂CHF₃ CH₂CH₃ 0 B-0315 H H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-0316 H H H H H CH₂CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0317 H H H H H CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0318 H H H H H CH₂CF₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-0319 H H H H H CH₂CF₂CF₂CF₂CF₂CF₂CF₂ CH₂CH₃ 0 B-0320 H H H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0321 H H H H H CH₂CF₂CF₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-0322 H H H H H CF₂CHFOCH₃ CH₂CH₃ 0 B-0323 H H H H H CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-0324 H H H H H CH₂CH₂OCH₃CF₃ CH₂CH₃ 0 B-0325 H H H H H CF₂CHFOCF₃ CH₂CH₃ 0 B-0326 H H H H H CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-0327 H H H H H CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-0328 H H H H H CH₂CH═CH₂ CH₂CH₃ 0 B-0329 H H H H H CH₂CH═CHCl CH₂CH₃ 0 B-0330 H H H H H CH₂CH═CCl₂ CH₂CH₃ 0 B-0331 H H H H H CH₂CH═C(CH₃)CF₃ CH₂CH₃ 0 B-0332 H H H H H CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-0333 H H H H H CH₂CH₂CH₂CF₂ CH₂CH₃ 0 B-0334 H H H H H CH₂C≡CH CH₂CH₃ 0 B-0335 H H H H H CH₂C≡CCH₃ CH₂CH₃ 0 B-0336 H H H H H CH₂C≡CC(CH₃)₃ CH₂CH₃ 0 B-0337 H H H H H CH₂C≡C(cyclopropyl) CH₂CH₃ 0 B-0338 H H H H H CH₂C≡CI CH₂CH₃ 0 B-0339 H H H H H CH₂C≡CCF₃ CH₂CH₃ 0 B-0340 H H H H H cyclopropyl CH₂CH₃ 0 B-0341 H H H H H cyclobutyl CH₂CH₃ 0 B-0342 H H H H H cyclopentyl CH₂CH₃ 0 B-0343 H H H H H cyclohexyl CH₂CH₃ 0 B-0344 H H H H H 4,4-difluorocyclohexyl CH₂CH₃ 0 B-0345 H H H H H 4-trifluoromethylcyclohexyl CH₂CH₃ 0 B-0346 H H H H H CH₂(cyclopropyl) CH₂CH₃ 0 B-0347 H H H H H CH₂(cyclobutyl) CH₂CH₃ 0 B-0348 H H H H H CH₂(cyclopentyl) CH₂CH₃ 0 B-0349 H H H H H CH₂(cyclohexyl) CH₂CH₃ 0 B-0350 H H H H H CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-0351 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-0352 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-0353 H H H H H CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-0354 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-0355 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-0356 H H H H H CH₂CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-0357 H H H H H CH₂SCH₃ CH₂CH₃ 0 B-0358 H H H H H CH₂SCH₂CH₃ CH₂CH₃ 0 B-0359 H H H H H CH₂CH₂SCH₃ CH₂CH₃ 0 B-0360 H H H H H CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-0361 H H H H H CH₂CH₂CH₂SCH₃ CH₂CH₃ 0

TABLE 100 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0362 H H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-0363 H H H H H CH(CH₃)SCH₃ CH₂CH₃ 0 B-0364 H H H H H CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-0365 H H H H H CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-0366 H H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-0367 H H H H H CH₂CH₂SCH(CH₃)₂ CH₂CH₃ 0 B-0368 H H H H H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-0369 H H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-0370 H H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-0371 H H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-0372 H H H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-0373 H H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-0374 H H H H H CH₂CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-0375 H H H H H CH₂CH₂CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-0376 H H H H H CH₂SOCH₃ CH₂CH₃ 0 B-0377 H H H H H CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0378 H H H H H CH₂CH₂SOCH₂CH₃ CH₂CH₃ 0 B-0379 H H H H H CH₂CH₂SOCH(CH₃)₂ CH₂CH₃ 0 B-0380 H H H H H CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0381 H H H H H CH(CH₃)SOCH₃ CH₂CH₃ 0 B-0382 H H H H H CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-0383 H H H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0384 H H H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-0385 H H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-0386 H H H H H CH₂CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0387 H H H H H CH₂CH₂CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0388 H H H H H CH₂SO₂CH₃ CH₂CH₃ 0 B-0389 H H H H H CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0390 H H H H H CH₂CH₂SO₂CH₂CH₃ CH₂CH₃ 0 B-0391 H H H H H CH₂CH₂SO₂CH(CH₃)₂ CH₂CH₃ 0 B-0392 H H H H H CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0393 H H H H H CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-0394 H H H H H CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-0395 H H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0396 H H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-0397 H H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-0398 H H H H H CH₂CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0399 H H H H H CH₂CH₂CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0400 H H H H H CH₂SCF₃ CH₂CH₃ 0 B-0401 H H H H H CH₂SCHF₂ CH₂CH₃ 0 B-0402 H H H H H CH₂SCH₂CF₃ CH₂CH₃ 0 B-0403 H H H H H CH₂SCH₂CHF₂ CH₂CH₃ 0 B-0404 H H H H H CH₂SCF₂CF₃ CH₂CH₃ 0 B-0405 H H H H H CH₂CH₂SCF₃ CH₂CH₃ 0 B-0406 H H H H H CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-0407 H H H H H CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-0408 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-0409 H H H H H CH(CH₃)SCF₃ CH₂CH₃ 0 B-0410 H H H H H CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-0411 H H H H H CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-0412 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-0413 H H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-0414 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-0415 H H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-0416 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-0417 H H H H H CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-0418 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-0419 H H H H H CH₂CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-0420 H H H H H CH₂CH₂CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-0421 H H H H H CH₂SOCF₃ CH₂CH₃ 0 B-0422 H H H H H CH₂CH₂SOCF₃ CH₂CH₃ 0

TABLE 101 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0423 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-0424 H H H H H CH(CH₃)SOCF₃ CH₂CH₃ 0 B-0425 H H H H H CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-0426 H H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-0427 H H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-0428 H H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-0429 H H H H H CH₂SO₂CF₃ CH₂CH₃ 0 B-0430 H H H H H CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-0431 H H H H H CH₂CH₂SO₃CH₂CF₃ CH₂CH₃ 0 B-0432 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-0433 H H H H H CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-0434 H H H H H CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-0435 H H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-0436 H H H H H CH₂CH(CH₃)CH₂SO₃CF₃ CH₂CH₃ 0 B-0437 H H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-0438 H H H H H CH₂C(═O)CH₃ CH₂CH₃ 0 B-0439 H H H H H CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-0440 H H H H H CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-0441 H H H H H CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-0442 H H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-0443 H H H H H CH₂C(═O)CF₃ CH₂CH₃ 0 B-0444 H H H H H CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-0445 H H H H H CH₂C(═O)OCH₃ CH₂CH₃ 0 B-0446 H H H H H CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-0447 H H H H H CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-0448 H H H H H CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-0449 H H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-0450 H H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-0451 H H H H H CH₂C(═O)NH₂ CH₂CH₃ 0 B-0452 H H H H H CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-0453 H H H H H CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-0454 H H H H H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-0455 H H H H H CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-0456 H H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-0457 H H H H H CH₂C(═O)NH(cyclopropyl) CH₂CH₃ 0 B-0458 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-0459 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-0460 H H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-0461 H H H H H CH₂CH₃C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-0462 H H H H H CH(CH₃)C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-0463 H H H H H CH(CH₃)C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-0464 H H H H H C(CH₃)₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-0465 H H H H H C(CH₃)₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-0466 H H H H H CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-0467 H H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-0468 H H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-0469 H H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-0470 H H H H H CH₂CH₂NHC(═O)OCH₃ CH₂CH₃ 0 B-0471 H H H H H CH₂CH₂NHC(═O)OC(CH₃)₃ CH₂CH₃ 0 B-0472 H H H H H CH₂CH₂CH₂NHC(═O)OCH₃ CH₂CH₃ 0 B-0473 H H H H H CH₂CH₂CH₂NHC(═O)OC(CH₃)₃ CH₂CH₃ 0 B-0474 H H H H H CH₂CH₂NHSO₂CHF₂ CH₂CH₃ 0 B-0475 H H H H H CH₂CH₂NHSO₂CF₃ CH₂CH₃ 0 B-0476 H H H H H CH₂CH₂CH₂NHSO₂CHF₃ CH₂CH₃ 0 B-0477 H H H H H CH₂CH₂CH₂NHSO₂CF₃ CH₂CH₃ 0 B-0478 H H H H H CH₂CH₂OH CH₂CH₃ 0 B-0479 H H H H H CH₂CH(OH)CH₃ CH₂CH₃ 0 B-0480 H H H H H CH₂CH₂CH₂OH CH₂CH₃ 0 B-0481 H H H H H CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-0482 H H H H H CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-0483 H H H H H CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0

TABLE 102 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0484 H H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-0485 H H H H H CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-0486 H H H H H CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-0487 H H H H H CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-0488 H H H H H CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-0489 H H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-0490 H H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-0491 H H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-0492 H H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-0493 H H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-0494 H H H H H CH₂Ph CH₂CH₃ 0 B-0495 H H H H H CH₂(2-F)Ph CH₂CH₃ 0 B-0496 H H H H H CH₂(3-F)Ph CH₂CH₃ 0 B-0497 H H H H H CH₂(4-F)Ph CH₂CH₃ 0 B-0498 H H H H H CH₂(2-Cl)Ph CH₂CH₃ 0 B-0499 H H H H H CH₂(3-Cl)Ph CH₂CH₃ 0 B-0500 H H H H H CH₂(4-Cl)Ph CH₂CH₃ 0 B-0501 H H H H H CH₂(2-CF₃)Ph CH₂CH₃ 0 B-0502 H H H H H CH₂(3-CF₃)Ph CH₂CH₃ 0 B-0503 H H H H H CH₂(4-CF₃)Ph CH₂CH₃ 0 B-0504 H H H H H CH₂(2-F-4-CF₃)Ph CH₂CH₃ 0 B-0505 H H H H H CH₂(naphthalen)-1-yl) CH₂CH₃ 0 B-0506 H H H H H CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-0507 H H H H H CH(CH₃)Ph CH₂CH₃ 0 B-0508 H H H H H CH₂CH₂Ph CH₂CH₃ 0 B-0509 H CF₃ H H H H H 0 B-0510 H CF₃ H H H CH₃ H 0 B-0511 H CF₃ H H H CH₂CH₃ H 0 B-0512 H CF₃ H H H CH(CH₃)₂ H 0 B-0513 H CF₃ H H H CH₂CH₂CH₃ H 0 B-0514 H CF₃ H H H CH₂CH(CH₃)₂ H 0 B-0515 H CF₃ H H H CH(CH₃)CH₂CH₃ H 0 B-0516 H CF₃ H H H CH₂C(CH₃)₃ H 0 B-0517 H CF₃ H H H CH₂(CH₂)₂CH₃ H 0 B-0518 H CF₃ H H H CH₂(CH₂)₃CH₃ H 0 B-0519 H CF₃ H H H CH₂(CH₂)₄CH₃ H 0 B-0520 H CF₃ H H H CH₂(CH₂)₆CH₃ H 0 B-0521 H CF₃ H H H CH₂OCH₃ H 0 B-0522 H CF₃ H H H CH₂OCH₂CH₃ H 0 B-0523 H CF₃ H H H CH₂CH₂OCH₃ H 0 B-0524 H CF₃ H H H CH₂CH₂OCH₂CH₃ H 0 B-0525 H CF₃ H H H CF₃ H 0 B-0526 H CF₃ H H H CHF₂ H 0 B-0527 H CF₃ H H H CH₂CF₃ H 0 B-0528 H CF₃ H H H CH₂CHF₂ H 0 B-0529 H CF₃ H H H CH₂CClF₂ H 0 B-0530 H CF₃ H H H CH₂CBrF₂ H 0 B-0531 H CF₃ H H H CF₂CF₃ H 0 B-0532 H CF₃ H H H CF₂CHF₂ H 0 B-0533 H CF₃ H H H CH₂CH₂CF₃ H 0 B-0534 H CF₃ H H H CH₂CF₂CF₃ H 0 B-0535 H CF₃ H H H CH₂CF₂CHF₂ H 0 B-0536 H CF₃ H H H CF₂CHFCF₃ H 0 B-0537 H CF₃ H H H CF₂CF₂CF₃ H 0 B-0538 H CF₃ H H H CH₂CF₂CF₂CF₃ H 0 B-0539 H CF₃ H H H CH₂CH₂CH₂CF₃ H 0 B-0540 H CF₃ H H H CH₂CF₂CHFCF₃ H 0 B-0541 H CF₃ H H H CH₂CH₂CF₂CF₃ H 0 B-0542 H CF₃ H H H CF₂CF₂CF₂CF₃ H 0 B-0543 H CF₃ H H H CH₂CH₂CH(CF₃)₂ H 0 B-0544 H CF₃ H H H CF₂CF₂CF₂CF₂CF₃ H 0

TABLE 103 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0545 H CF₃ H H H CH₂CF₂CF₂CF₂CF₃ H 0 B-0546 H CF₃ H H H CH₂CH₂CH₂CH₂CF₃ H 0 B-0547 H CF₃ H H H CH₂CF₂CF₂CF₂CHF₂ H 0 B-0548 H CF₃ H H H CH₂CF₂CF(CF₃)CF₂C(CR₃)₃ H 0 B-0549 H CF₃ H H H CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-0550 H CF₃ H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-0551 H CF₃ H H H CF₂CHFOCH₃ H 0 B-0552 H CF₃ H H H CF₂CHFOCH₂CH₃ H 0 B-0553 H CF₃ H H H CH₂CH₂OCH₂CF₃ H 0 B-0554 H CF₃ H H H CF₂CHFOCF₃ H 0 B-0555 H CF₃ H H H CF₂CHFOCF₂CF₃ H 0 B-0556 H CF₃ H H H CH₂CHFOCF₂CF₂CF₃ H 0 B-0557 H CF₃ H H H CH₂CH═CH₂ H 0 B-0558 H CF₃ H H H CH₂CH═CHCl H 0 B-0559 H CF₃ H H H CH₂CH═CCl₂ H 0 B-0560 H CF₃ H H H CH₂CH₂CF═CF₂ H 0 B-0561 H CF₃ H H H CH₂CH₂CH═CF₂ H 0 B-0562 H CF₃ H H H CH₂C≡CH H 0 B-0563 H CF₃ H H H CH₂C≡CCH₃ H 0 B-0564 H CF₃ H H H CH₂C≡CI H 0 B-0565 H CF₃ H H H CH₂C≡CCF₃ H 0 B-0566 H CF₃ H H H cyclobutyl H 0 B-0567 H CF₃ H H H cyclopentyl H 0 B-0568 H CF₃ H H H cyclohexyl H 0 B-0569 H CF₃ H H H 4,4-difluorocyclohexyl H 0 B-0570 H CF₃ H H H CH₂(cyclopropyl) H 0 B-0571 H CF₃ H H H CH₂(cyclobutyl) H 0 B-0572 H CF₃ H H H CH₂(cyclopentyl) H 0 B-0573 H CF₃ H H H CH₂CH₂(cyclopropyl) H 0 B-0574 H CF₃ H H H CH₂(2,2-difluorocyclopropyl) H 0 B-0575 H CF₃ H H H CH₂(2,2-dichlorocydopropyl) H 0 B-0576 H CF₃ H H H CH₂(4,4-difluorccyclohexyl) H 0 B-0577 H CF₃ H H H CH₂CH₃(2,2-difluorocyclopropyl) H 0 B-0578 H CF₃ H H H CH₂CH₃(2,2-dichlorocyclopropyl) H 0 B-0579 H CF₃ H H H CH₂SCH₃ H 0 B-0580 H CF₃ H H H CH₂SCH₂CH₃ H 0 B-0581 H CF₃ H H H CH₂CH₂SCH₃ H 0 B-0582 H CF₃ H H H CH₂CH₃SCH₂CH₃ H 0 B-0583 H CF₃ H H H CH₂CH₂CH₂SCH₃ H 0 B-0584 H CF₃ H H H CH₂CH₂CH₂SCH₂CH₃ H 0 B-0585 H CF₃ H H H CH(CH₃)SCH₃ H 0 B-0586 H CF₃ H H H CH(CH₃)SCH₂CH₃ H 0 B-0587 H CF₃ H H H CH₂CH(CH₃)SCH₃ H 0 B-0588 H CF₃ H H H CH₂CH(CH₃)SCH₂CH₃ H 0 B-0589 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₃ H 0 B-0590 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-0591 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₃ H 0 B-0592 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-0593 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₃ H 0 B-0594 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-0595 H CF₃ H H H CH₂SOCH₃ H 0 B-0596 H CF₃ H H H CH₂CH₂SOCH₃ H 0 B-0597 H CF₃ H H H CH₂CH₂CH₃SOCH₃ H 0 B-0598 H CF₃ H H H CH(CH₃)SOCH₃ H 0 B-0599 H CF₃ H H H CH₂CH(CH₃)SOCH₃ H 0 B-0600 H CF₃ H H H CH(CH₃)CH₂CH₂SOCH₃ H 0 B-0601 H CF₃ H H H CH₂CH(CH₃)CH₂SOCH₃ H 0 B-0602 H CF₃ H H H CH₂CH₂CH(CH₃)SOCH₃ H 0 B-0603 H CF₃ H H H CH₂SO₂CH₃ H 0 B-0604 H CF₃ H H H CH₂CH₂SO₂CH₃ H 0 B-0605 H CF₃ H H H CH₂CH₂CH₂SO₂CH₃ H 0

TABLE 104 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0606 H CF₃ H H H CH(CH₃)SO₂CH₃ H 0 B-0607 H CF₃ H H H CH₂CH(CH₃)SO₂CH₃ H 0 B-0608 H CF₃ H H H CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-0609 H CF₃ H H H CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-0610 H CF₃ H H H CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-0611 H CF₃ H H H CH₂SCF₃ H 0 B-0612 H CF₃ H H H CH₂SCHF₂ H 0 B-0613 H CF₃ H H H CH₂SCH₂CF₃ H 0 B-0614 H CF₃ H H H CH₂SCH₂CHF₂ H 0 B-0615 H CF₃ H H H CH₂SCF₂CF₃ H 0 B-0616 H CF₃ H H H CH₂CH₂SCF₃ H 0 B-0617 H CF₃ H H H CH₂CH₂SCH₂CF₃ H 0 B-0618 H CF₃ H H H CH₂CH₂CH₂SCF₃ H 0 B-0619 H CF₃ H H H CH₂CH₂CH₂SCH₂CF₃ H 0 B-0620 H CF₃ H H H CH(CH₃)SCF₃ H 0 B-0621 H CF₃ H H H CH(CH₃)SCH₂CF₃ H 0 B-0622 H CF₃ H H H CH₃CH(CH₃)SCF₃ H 0 B-0623 H CF₃ H H H CH₂CH(CH₃)SCH₂CF₃ H 0 B-0624 H CF₃ H H H CH(CH₃)CH₂CH₂SCF₃ H 0 B-0625 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-0626 H CF₃ H H H CH₂CH(CH₃)CH₂SCF₃ H 0 B-0627 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-0628 H CF₃ H H H CH₂CH₂CH(CH₃)SCF₃ H 0 B-0629 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-0630 H CF₃ H H H CH₂SOCF3 H 0 B-0631 H CF₃ H H H CH₂CH₂SOCF₃ H 0 B-0632 H CF₃ H H H CH₂CH₂CH₂SOCF₃ H 0 B-0633 H CF₃ H H H CH(CH₃)SOCF₃ H 0 B-0634 H CF₃ H H H CH₂CH(CH₃)SOCF₃ H 0 B-0635 H CF₃ H H H CH(CH₃)CH₂CH₂SOCF₃ H 0 B-0636 H CF₃ H H H CH₂CH(CH₃)CH₂SOCF₃ H 0 B-0637 H CF₃ H H H CH₂CH₂CH(CH₃)SOCF₃ H 0 B-0638 H CF₃ H H H CH₂SO₂CF₃ H 0 B-0639 H CF₃ H H H CH₂CH₂SO₂CF₃ H 0 B-0640 H CF₃ H H H CH₂CH₂CH₂SO₂CF₃ H 0 B-0641 H CF₃ H H H CH(CH₃)SO₂CF₃ H 0 B-0642 H CF₃ H H H CH₂CH(CH₃)SO₂CF₃ H 0 B-0643 H CF₃ H H H CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-0644 H CF₃ H H H CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-0645 H CF₃ H H H CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-0646 H CF₃ H H H CH₂C(═O)CH₃ H 0 B-0647 H CF₃ H H H CH₂C(═O)CH₂CH₃ H 0 B-0648 H CF₃ H H H CH₂C(═O)C(CH₃)₃ H 0 B-0649 H CF₃ H H H CH₂CH₂C(═O)CH₃ H 0 B-0650 H CF₃ H H H CH₂CH₂C(═O)C(CH₃)₃ H 0 B-0651 H CF₃ H H H CH₂C(═O)CF₃ H 0 B-0652 H CF₃ H H H CH₂CH₂C(═O)CF₃ H 0 B-0653 H CF₃ H H H CH₂C(═O)OCH₃ H 0 B-0654 H CF₃ H H H CH₂C(═O)OCH₂CH₃ H 0 B-0655 H CF₃ H H H CH₂C(═O)OC(CH₃)₃ H 0 B-0656 H CF₃ H H H CH₂CH₂C(═O)OCH₃ H 0 B-0657 H CF₃ H H H CH₂CH₂C(═O)OCH₂CH₃ H 0 B-0658 H CF₃ H H H CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-0659 H CF₃ H H H CH₂C(═O)NH₂ H 0 B-0660 H CF₃ H H H CH₂CH₂C(═O)NH₂ H 0 B-0661 H CF₃ H H H CH₂C(═O)NHCH₃ H 0 B-0662 H CF₃ H H H CH₂C(═O)NHCH(CH₃)₂ H 0 B-0663 H CF₃ H H H CH₂CH₂C(═O)NHCH₃ H 0 B-0664 H CF₃ H H H CH₂CH₂C(O)NHCH(CH₃)₂ H 0 B-0665 H CF₃ H H H CH₂C(═O)NHCH₂CHF₂ H 0 B-0666 H CF₃ H H H CH₂C(═O)NHCH₂CF₃ H 0

TABLE 105 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0667 H CF₃ H H H CH₂CH₂C(═O)NHCH₂CHF₂ H 0 B-0668 H CF₃ H H H CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-0669 H CF₃ H H H CH₂C(═O)N(CH₃)₂ H 0 B-0670 H CF₃ H H H CH₂C(═O)N(CH₂CH₃)₂ H 0 B-0671 H CF₃ H H H CH₂CH₂C(═O)N(CH₃)₂ H 0 B-0672 H CF₃ H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-0673 H CF₃ H H H CH₂CH₂OH H 0 B-0674 H CF₃ H H H CH₂CH(OH)CH₃ H 0 B-0675 H CF₃ H H H CH₂CH₂CH₂OH H 0 B-0676 H CF₃ H H H CH₂CH(OH)CH₂CH₃ H 0 B-0677 H CF₃ H H H CH₂CH(OH)C(CH₃)₃ H 0 B-0678 H CF₃ H H H CH₂CH₂CH(OH)CH₃ H 0 B-0679 H CF₃ H H H CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-0680 H CF₃ H H H CH₂C(═NOH)CH₃ H 0 B-0681 H CF₃ H H H CH₂C(═NOH)CH₂CH₃ H 0 B-0682 H CF₃ H H H CH₂C(═NOH)C(CH₃)₃ H 0 B-0683 H CF₃ H H H CH₂C(═NOCH₃)CH₂ H 0 B-0684 H CF₃ H H H CH₂C(═NOCH₂)CH₂CH₃ H 0 B-0685 H CF₃ H H H CH₂C(═NOCH₂CH₃)CH₃ H 0 B-0686 H CF₃ H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-0687 H CF₃ H H H CH₂C(═NOCH₂CF₃)CH₃ H 0 B-0688 H CF₃ H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0 B-0689 H CF₃ H H H CH₂Ph H 0 B-0690 H CF₃ H H H CH₂(2-F)Ph H 0 B-0691 H CF₃ H H H CH₂(3-F)Ph H 0 B-0692 H CF₃ H H H CH₂(4-F)Ph H 0 B-0693 H CF₃ H H H CH₂(2-Cl)Ph H 0 B-0694 H CF₃ H H H CH₂(3-Cl)Ph H 0 B-0695 H CF₃ H H H CH₂(4-Cl)Ph H 0 B-0696 H CF₃ H H H CH₂(2-CF₃)Ph H 0 B-0697 H CF₃ H H H CH₂(3-CF₃)Ph H 0 B-0698 H CF₃ H H H CH₂(4-CF₃)Ph H 0 B-0699 H CF₃ H H H CH₂(naphthalene-1-yl) H 0 B-0700 H CF₃ H H H CH₂(naphthalen-2-yl) H 0 B-0701 H CF₃ H H H CH₂CH₂Ph H 0 B-0702 H CF₃ H H H H CH₂CH₃ 0 B-0703 H CF₃ H H H CH₃ CH₂CH₃ 0 B-0704 H CF₃ H H H CH₂CH₃ CH₂CH₃ 0 B-0705 H CF₃ H H H CH(CH₃)₂ CH₂CH₃ 0 B-0706 H CF₃ H H H CH₂CH₂CH₃ CH₂CH₃ 0 B-0707 H CF₃ H H H CH₂CH(CH₃)₂ CH₂CH₃ 0 B-0708 H CF₃ H H H CH₂C(CH₃)₃ CH₂CH₃ 0 B-0709 H CF₃ H H H CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-0710 H CF₃ H H H CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-0711 H CF₃ H H H CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-0712 H CF₃ H H H CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-0713 H CF₃ H H H CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-0714 H CF₃ H H H CH₂OCH₃ CH₂CH₃ 0 B-0715 H CF₃ H H H CH₂OCH₂CH₃ CH₂CH₃ 0 B-0716 H CF₃ H H H CH₂CH₂OCH₃ CH₂CH₃ 0 B-0717 H CF₃ H H H CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-0718 H CF₃ H H H CF₃ CH₂CH₃ 0 B-0719 H CF₃ H H H CHF₂ CH₂CH₃ 0 B-0720 H CF₃ H H H CH₂CF₃ CH₂CH₃ 0 B-0721 H CF₃ H H H CH₂CHF₂ CH₂CH₃ 0 B-0722 H CF₃ H H H CH₂CClF₂ CH₂CH₃ 0 B-0723 H CF₃ H H H CH₂CBrF₂ CH₂CH₃ 0 B-0724 H CF₃ H H H CF₂CF₃ CH₂CH₃ 0 B-0725 H CF₃ H H H CF₂CHF₂ CH₂CH₃ 0 B-0726 H CF₃ H H H CH₂CH₂CF₃ CH₂CH₃ 0 B-0727 H CF₃ H H H CH₂CF₂CF₃ CH₂CH₃ 0

TABLE 106 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0728 H CF₃ H H H CH₂CF₂CHF₂ CH₂CH₃ 0 B-0729 H CF₃ H H H CF₂CHFCF₃ CH₂CH₃ 0 B-0730 H CF₃ H H H CF₂CF₂CF₃ CH₂CH₃ 0 B-0731 H CF₃ H H H CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0732 H CF₃ H H H CH₂CF₂CHFCF₃ CH₂CH₃ 0 B-0733 H CF₃ H H H CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0734 H CF₃ H H H CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-0735 H CF₃ H H H CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0736 H CF₃ H H H CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-0737 H CF₃ H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0738 H CF₃ H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-0739 H CF₃ H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0740 H CF₃ H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-0741 H CF₃ H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-0742 H CF₃ H H H CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0743 H CF₃ H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-0744 H CF₃ H H H CF₂CHFOCH₃ CH₂CH₃ 0 B-0745 H CF₃ H H H CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-0746 H CF₃ H H H CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-0747 H CF₃ H H H CF₂CHFOCF₃ CH₂CH₃ 0 B-0748 H CF₃ H H H CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-0749 H CF₃ H H H CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-0750 H CF₃ H H H CH₂CH═CH₂ CH₂CH₃ 0 B-0751 H CF₃ H H H CH₂CH═CHCl CH₂CH₃ 0 B-0752 H CF₃ H H H CH₂CH═CCl₂ CH₂CH₃ 0 B-0753 H CF₃ H H H CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-0754 H CF₃ H H H CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-0755 H CF₃ H H H CH₂C≡CH CH₂CH₃ 0 B-0756 H CF₃ H H H CH₂C≡CCH₃ CH₂CH₃ 0 B-0757 H CF₃ H H H CH₂C≡CI CH₂CH₃ 0 B-0758 H CF₃ H H H CH₂C≡CCF₃ CH₂CH₃ 0 B-0759 H CF₃ H H H cyclobutyl CH₂CH₃ 0 B-0760 H CF₃ H H H cyclopentyl CH₂CH₃ 0 B-0761 H CF₃ H H H cyclohexyl CH₂CH₃ 0 B-0762 H CF₃ H H H 4,4-difluorocyclohexyl CH₂CH₃ 0 B-0763 H CF₃ H H H CH₂(cyclopropyl) CH₂CH₃ 0 B-0764 H CF₃ H H H CH₂(cyclobutyl) CH₂CH₃ 0 B-0765 H CF₃ H H H CH₂(cyclopentyl) CH₂CH₃ 0 B-0766 H CF₃ H H H CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-0767 H CF₃ H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-0768 H CF₃ H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-0769 H CF₃ H H H CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-0770 H CF₃ H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-0771 H CF₃ H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-0772 H CF₃ H H H CH₂SCH₃ CH₂CH₃ 0 B-0773 H CF₃ H H H CH₂SCH₂CH₃ CH₂CH₃ 0 B-0774 H CF₃ H H H CH₂CH₂SCH₃ CH₂CH₃ 0 B-0775 H CF₃ H H H CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-0776 H CF₃ H H H CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-0777 H CF₃ H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-0778 H CF₃ H H H CH(CH₃)SCH₃ CH₂CH₃ 0 B-0779 H CF₃ H H H CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-0780 H CF₃ H H H CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-0781 H CF₃ H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-0782 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-0783 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-0784 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-0785 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-0786 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-0787 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-0788 H CF₃ H H H CH₂SOCH₃ CH₂CH₃ 0

TABLE 107 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0789 H CF₃ H H H CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0790 H CF₃ H H H CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0791 H CF₃ H H H CH(CH₃)SOCH₃ CH₂CH₃ 0 B-0792 H CF₃ H H H CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-0793 H CF₃ H H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-0794 H CF₃ H H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-0795 H CF₃ H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-0796 H CF₃ H H H CH₂SO₂CH₃ CH₂CH₃ 0 B-0797 H CF₃ H H H CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0798 H CF₃ H H H CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0799 H CF₃ H H H CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-0800 H CF₃ H H H CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-0801 H CF₃ H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-0802 H CF₃ H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-0803 H CF₃ H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-0804 H CF₃ H H H CH₂SCF₃ CH₂CH₃ 0 B-0805 H CF₃ H H H CH₂SCHF₂ CH₂CH₃ 0 B-0806 H CF₃ H H H CH₂SCH₂CF₃ CH₂CH₃ 0 B-0807 H CF₃ H H H CH₂SCH₂CHF₂ CH₂CH₃ 0 B-0808 H CF₃ H H H CH₂SCF₂CF₃ CH₂CH₃ 0 B-0809 H CF₃ H H H CH₂CH₂SCF₃ CH₂CH₃ 0 B-0810 H CF₃ H H H CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-0811 H CF₃ H H H CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-0812 H CF₃ H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-0813 H CF₃ H H H CH(CH₃)SCF₃ CH₂CH₃ 0 B-0814 H CF₃ H H H CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-0815 H CF₃ H H H CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-0816 H CF₃ H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-0817 H CF₃ H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-0818 H CF₃ H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-0819 H CF₃ H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-0820 H CF₃ H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-0821 H CF₃ H H H CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-0822 H CF₃ H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-0823 H CF₃ H H H CH₂SOCF₃ CH₂CH₃ 0 B-0824 H CF₃ H H H CH₂CH₂SOCF₃ CH₂CH₃ 0 B-0825 H CF₃ H H H CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-0826 H CF₃ H H H CH(CH₃)SOCF₃ CH₂CH₃ 0 B-0827 H CF₃ H H H CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-0828 H CF₃ H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-0829 H CF₃ H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-0830 H CF₃ H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-0831 H CF₃ H H H CH₂SO₂CF₃ CH₂CH₃ 0 B-0832 H CF₃ H H H CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-0833 H CF₃ H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-0834 H CF₃ H H H CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-0835 H CF₃ H H H CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-0836 H CF₃ H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-0837 H CF₃ H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-0838 H CF₃ H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-0839 H CF₃ H H H CH₂C(═O)CH₃ CH₂CH₃ 0 B-0840 H CF₃ H H H CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-0841 H CF₃ H H H CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-0842 H CF₃ H H H CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-0843 H CF₃ H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-0844 H CF₃ H H H CH₂C(═O)CF₃ CH₂CH₃ 0 B-0845 H CF₃ H H H CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-0846 H CF₃ H H H CH₂C(═O)OCH₃ CH₂CH₃ 0 B-0847 H CF₃ H H H CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-0848 H CF₃ H H H CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-0849 H CF₃ H H H CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0

TABLE 108 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0850 H CF₃ H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-0851 H CF₃ H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-0852 H CF₃ H H H CH₂C(═O)NH₂ CH₂CH₃ 0 B-0853 H CF₃ H H H CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-0854 H CF₃ H H H CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-0855 H CF₃ H H H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-0856 H CF₃ H H H CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-0857 H CF₃ H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-0858 H CF₃ H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-0859 H CF₃ H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-0860 H CF₃ H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-0861 H CF₃ H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-0862 H CF₃ H H H CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-0863 H CF₃ H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-0864 H CF₃ H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-0865 H CF₃ H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-0866 H CF₃ H H H CH₂CH₂OH CH₂CH₃ 0 B-0867 H CF₃ H H H CH₂CH(OH)CH₃ CH₂CH₃ 0 B-0868 H CF₃ H H H CH₂CH₂CH₂OH CH₂CH₃ 0 B-0869 H CF₃ H H H CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-0870 H CF₃ H H H CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-0871 H CF₃ H H H CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0 B-0872 H CF₃ H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-0873 H CF₃ H H H CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-0874 H CF₃ H H H CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-0875 H CF₃ H H H CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-0876 H CF₃ H H H CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-0877 H CF₃ H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-0878 H CF₃ H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-0879 H CF₃ H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-0880 H CF₃ H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-0881 H CF₃ H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-0882 H CF₃ H H H CH₂Ph CH₂CH₃ 0 B-0883 H CF₃ H H H CH₂(2-F)Ph CH₂CH₃ 0 B-0884 H CF₃ H H H CH₂(3-F)Ph CH₂CH₃ 0 B-0885 H CF₃ H H H CH₂(4-F)Ph CH₂CH₃ 0 B-0886 H CF₃ H H H CH₂(2-Cl)Ph CH₂CH₃ 0 B-0887 H CF₃ H H H CH₂(3-Cl)Ph CH₂CH₃ 0 B-0888 H CF₃ H H H CH₂(4-Cl)Ph CH₂CH₃ 0 B-0889 H CF₃ H H H CH₂(2-CF₃)Ph CH₂CH₃ 0 B-0890 H CF₃ H H H CH₂(3-CF₃)Ph CH₂CH₃ 0 B-0891 H CF₃ H H H CH₂(4-CF₃)Ph CH₂CH₃ 0 B-0892 H CF₃ H H H CH₂(naphthalen-1-yl) CH₂CH₃ 0 B-0893 H CF₃ H H H CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-0894 H CF₃ H H H CH₂CH₂Ph CH₂CH₃ 0 B-0895 H H F H H H H 0 B-0896 H H F H H CH₃ H 0 B-0897 H H F H H CH₂CH₃ H 0 B-0898 H H F H H CH(CH₃)₂ H 0 B-0899 H H F H H CH₂CH₂CH₃ H 0 B-0900 H H F H H CH₂CH(CH₃)₂ H 0 B-0901 H H F H H CH₂C(CH₃)₃ H 0 B-0902 H H F H H CH(CH₃)CH₂CH₃ H 0 B-0903 H H F H H CH₂(CH₂)₂CH₃ H 0 B-0904 H H F H H CH₂(CH₂)₃CH₃ H 0 B-0905 H H F H H CH₂(CH₂)₄CH₃ H 0 B-0906 H H F H H CH₂(CH₂)₆CH₃ H 0 B-0907 H H F H H CH₂OCH₃ H 0 B-0908 H H F H H CH₂OCH₂CH₃ H 0 B-0909 H H F H H CH₂CH₂OCH₃ H 0 B-0910 H H F H H CH₂CH₂OCH₂CH₃ H 0

TABLE 109 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0911 H H F H H CF₃ H 0 B-0912 H H F H H CHF₂ H 0 B-0913 H H F H H CH₂CF₃ H 0 B-0914 H H F H H CH₂CHF₂ H 0 B-0915 H H F H H CH₂CClF₂ H 0 B-0916 H H F H H CH₂CBrF₂ H 0 B-0917 H H F H H CF₂CF₃ H 0 B-0918 H H F H H CF₂CHF₂ H 0 B-0919 H H F H H CH₂CH₃CF₃ H 0 B-0920 H H F H H CH₂CF₂CF₃ H 0 B-0921 H H F H H CH₂CF₂CHF₂ H 0 B-0922 H H F H H CF₂CHFCF₃ H 0 B-0923 H H F H H CF₂CF₂CF₃ H 0 B-0924 H H F H H CH₂CF₂CF₂CF₃ H 0 B-0925 H H F H H CH₂CF₂CHFCF₃ H 0 B-0926 H H F H H CH₂CH₃CH₂CF₃ H 0 B-0927 H H F H H CH₂CH₂CF₂CF₃ H 0 B-0928 H H F H H CF₂CF₂CF₂CF₃ H 0 B-0929 H H F H H CH₂CH₂CH(CF₃)₂ H 0 B-0930 H H F H H CF₂CF₂CF₂CF₂CF₃ H 0 B-0931 H H F H H CH₂CF₂CF₂CF₂CF₃ H 0 B-0932 H H F H H CH₂CH₂CH₂CH₂CF₃ H 0 B-0933 H H F H H CH₂CF₂CF₂CF₂CHF₂ H 0 B-0934 H H F H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-0935 H H F H H CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-0936 H H F H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-0937 H H F H H CF₂CHFOCH₃ H 0 B-0938 H H F H H CF₂CHFOCH₂CH₃ H 0 B-0939 H H F H H CH₂CH₂OCH₂CF₃ H 0 B-0940 H H F H H CF₂CHFOCF₃ H 0 B-0941 H H F H H CF₂CHFOCF₂CF₃ H 0 B-0942 H H F H H CF₂CHFOCF₂CF₂CF₃ H 0 B-0943 H H F H H CH₂CH═CH₂ H 0 B-0944 H H F H H CH₂CH═CHCl H 0 B-0945 H H F H H CH₂CH═CCl₂ H 0 B-0946 H H F H H CH₂CH₂CF═CF₂ H 0 B-0947 H H F H H CH₂CH₂CH═CF₂ H 0 B-0948 H H F H H CH₂C≡CH H 0 B-0949 H H F H H CH₂C≡CCH₃ H 0 B-0950 H H F H H CH₂C≡CI H 0 B-0951 H H F H H CH₂C≡CCF₃ H 0 B-0952 H H F H H cyclobutyl H 0 B-0953 H H F H H cyclopentyl H 0 B-0954 H H F H H cyclohexyl H 0 B-0955 H H F H H 4,4-difluorocyclohexyl H 0 B-0956 H H F H H CH₂(cyclopropyl) H 0 B-0957 H H F H H CH₂(cyclobutyl) H 0 B-0958 H H F H H CH₂(cyclopentyl) H 0 B-0959 H H F H H CH₂CH₂(cyclopropyl) H 0 B-0960 H H F H H CH₂(2,2-difluorocyclopropyl) H 0 B-0961 H H F H H CH₂(2,2-dichlorocyclopropyl) H 0 B-0962 H H F H H CH₂(4,4-difluorocyclohexyl) H 0 B-0963 H H F H H CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-0964 H H F H H CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-0965 H H F H H CH₂SCH₃ H 0 B-0966 H H F H H CH₂SCH₂CH₃ H 0 B-0967 H H F H H CH₂CH₂SCH₃ H 0 B-0968 H H F H H CH₂CH₂SCH₂CH₃ H 0 B-0969 H H F H H CH₂CH₂CH₂SCH₃ H 0 B-0970 H H F H H CH₂CH₂CH₂SCH₂CH₃ H 0 B-0971 H H F H H CH(CH₃)SCH₃ H 0

TABLE 110 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-0972 H H F H H CH(CH₃)SCH₂CH₃ H 0 B-0973 H H F H H CH₂CH(CH₃)SCH₃ H 0 B-0974 H H F H H CH₂CH(CH₃)SCH₂CH₃ H 0 B-0975 H H F H H CH(CH₃)CH₂CH₂SCH₃ H 0 B-0976 H H F H H CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-0977 H H F H H CH₂CH(CH₃)CH₂SCH₃ H 0 B-0978 H H F H H CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-0979 H H F H H CH₂CH₂CH(CH₃)SCH₃ H 0 B-0980 H H F H H CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-0981 H H F H H CH₂SOCH₃ H 0 B-0982 H H F H H CH₂CH₂SOCH₃ H 0 B-0983 H H F H H CH₂CH₂CH₂SOCH₃ H 0 B-0984 H H F H H CH(CH₃)SOCH₃ H 0 B-0985 H H F H H CH₂CH(CH₃)SOCH₃ H 0 B-0986 H H F H H CH(CH₃)CH₂CH₂SOCH₃ H 0 B-0987 H H F H H CH₂CH(CH₃)CH₂SOCH₃ H 0 B-0988 H H F H H CH₂CH₂CH(CH₃)SOCH₃ H 0 B-0989 H H F H H CH₂SO₂CH₃ H 0 B-0990 H H F H H CH₂CH₂SO₂CH₃ H 0 B-0991 H H F H H CH₂CH₂CH₂SO₂CH₃ H 0 B-0992 H H F H H CH(CH₃)SO₂CH₃ H 0 B-0993 H H F H H CH₂CH(CH₃)SO₂CH₃ H 0 B-0994 H H F H H CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-0995 H H F H H CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-0996 H H F H H CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-0997 H H F H H CH₂SCF₃ H 0 B-0998 H H F H H CH₂SCHF₂ H 0 B-0999 H H F H H CH₂SCH₂CF₃ H 0 B-1000 H H F H H CH₂SCH₂CHF₂ H 0 B-1001 H H F H H CH₂SCF₂CF₃ H 0 B-1002 H H F H H CH₂CH₂SCF₃ H 0 B-1003 H H F H H CH₂CH₂SCH₂CF₃ H 0 B-1004 H H F H H CH₂CH₂CH₂SCF₃ H 0 B-1005 H H F H H CH₂CH₂CH₂SCH₂CF₃ H 0 B-1006 H H F H H CH(CH₃)SCF₃ H 0 B-1007 H H F H H CH(CH₃)SCH₂CF₃ H 0 B-1008 H H F H H CH₂CH(CH₃)SCF₃ H 0 B-1009 H H F H H CH₂CH(CH₃)SCH₂CF₃ H 0 B-1010 H H F H H CH(CH₃)CH₂CH₂SCF₃ H 0 B-1011 H H F H H CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-1012 H H F H H CH₂CH(CH₃)CH₂SCF₃ H 0 B-1013 H H F H H CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-1014 H H F H H CH₂CH₂CH(CH₃)SCF₃ H 0 B-1015 H H F H H CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-1016 H H F H H CH₂SOCF₃ H 0 B-1017 H H F H H CH₂CH₂SOCF₃ H 0 B-1018 H H F H H CH₂CH₂CH₂SOCF₃ H 0 B-1019 H H F H H CH(CH₃)SOCF₃ H 0 B-1020 H H F H H CH₂CH(CH₃)SOCF₃ H 0 B-1021 H H F H H CH(CH₃)CH₂CH₂SOCF₃ H 0 B-1022 H H F H H CH₂CH(CH₃)CH₂SOCF₃ H 0 B-1023 H H F H H CH₂CH₂CH(CH₃)SOCF₃ H 0 B-1024 H H F H H CH₂SO₂CF₃ H 0 B-1025 H H F H H CH₂CH₂SO₂CF₃ H 0 B-1026 H H F H H CH₂CH₂CH₂SO₂CF₃ H 0 B-1027 H H F H H CH(CH₃)SO₂CF₃ H 0 B-1028 H H F H H CH₂CH(CH₃)SO₂CF₃ H 0 B-1029 H H F H H CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-1030 H H F H H CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-1031 H H F H H CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-1032 H H F H H CH₂C(═O)CH₃ H 0

TABLE 111 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1033 H H F H H CH₂C(═O)CH₂CH₃ H 0 B-1034 H H F H H CH₂C(═O)C(CH₃)₃ H 0 B-1035 H H F H H CH₂CH₂C(═O)CH₃ H 0 B-1036 H H F H H CH₂CH₂C(═O)C(CH₃)₃ H 0 B-1037 H H F H H CH₂C(═O)CF₃ H 0 B-1038 H H F H H CH₂CH₂C(═O)CF₃ H 0 B-1039 H H F H H CH₂C(═O)OCH₃ H 0 B-1040 H H F H H CH₂C(═O)OCH₂CH₃ H 0 B-1041 H H F H H CH₂C(═O)OC(CH₃)₃ H 0 B-1042 H H F H H CH₂CH₂C(═O)OCH₃ H 0 B-1043 H H F H H CH₂CH₂C(═O)OCH₂CH₃ H 0 B-1044 H H F H H CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-1045 H H F H H CH₂C(═O)NH₂ H 0 B-1046 H H F H H CH₂CH₂C(═O)NH₂ H 0 B-1047 H H F H H CH₂C(═O)NHCH₃ H 0 B-1048 H H F H H CH₂C(═O)NHCH(CH₃)₂ H 0 B-1049 H H F H H CH₂CH₂C(═O)NHCH₃ H 0 B-1050 H H F H H CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-1051 H H F H H CH₂C(═O)NHCH₂CHF₂ H 0 B-1052 H H F H H CH₂C(═O)NHCH₂CF₃ H 0 B-1053 H H F H H CH₂CH₂C(═O)NHCH₂CHF₂ H 0 B-1054 H H F H H CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-1055 H H F H H CH₂C(═O)N(CH₃)₂ H 0 B-1056 H H F H H CH₂C(═O)N(CH₂CH₃)₂ H 0 B-1057 H H F H H CH₂CH₂C(═O)N(CH₃)₂ H 0 B-1058 H H F H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-1059 H H F H H CH₂CH₂OH H 0 B-1060 H H F H H CH₂CH(OH)CH₃ H 0 B-1061 H H F H H CH₂CH₂CH₂OH H 0 B-1062 H H F H H CH₃CH(OH)CH₂CH₃ H 0 B-1063 H H F H H CH₂CH(OH)C(CH₃)₃ H 0 B-1064 H H F H H CH₂CH₂CH(OH)CH₃ H 0 B-1065 H H F H H CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-1066 H H F H H CH₂C(═NOH)CH₃ H 0 B-1067 H H F H H CH₂C(═NOH)CH₂CH₃ H 0 B-1068 H H F H H CH₂C(═NOH)C(CH₃)₃ H 0 B-1069 H H F H H CH₂C(═NOCH₃)CH₃ H 0 B-1070 H H F H H CH₂C(═NOCH₃)CH₂CH₃ H 0 B-1071 H H F H H CH₂C(═NOCH₂CH₃)CH₃ H 0 B-1072 H H F H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-1073 H H F H H CH₂C(═NOCH₂CF₃)CH₃ H 0 B-1074 H H F H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0 B-1075 H H F H H CH₂Ph H 0 B-1076 H H F H H CH₂(2-F)Ph H 0 B-1077 H H F H H CH₂(3-F)Ph H 0 B-1078 H H F H H CH₂(4-F)Ph H 0 B-1079 H H F H H CH₂(2-Cl)Ph H 0 B-1080 H H F H H CH₂(3-Cl)Ph H 0 B-1081 H H F H H CH₂(4-Cl)Ph H 0 B-1082 H H F H H CH₂(2-CF₃)Ph H 0 B-1083 H H F H H CH₂(3-CF₃)Ph H 0 B-1084 H H F H H CH₂(4-CF₃)Ph H 0 B-1085 H H F H H CH₂(naphthalen-1-yl) H 0 B-1086 H H F H H CH₂(naphthaLen-2-yl) H 0 B-1087 H H F H H CH₂CH₂Ph H 0 B-1088 H H F H H H CH₂CH₃ 0 B-1089 H H F H H CH₃ CH₂CH₃ 0 B-1090 H H F H H CH₂CH₃ CH₂CH₃ 0 B-1091 H H F H H CH(CH₃)₂ CH₂CH₃ 0 B-1092 H H F H H CH₂CH₂CH₃ CH₂CH₃ 0 B-1093 H H F H H CH₂CH(CH₃)₂ CH₂CH₃ 0

TABLE 112 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1094 H H F H H CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-1095 H H F H H CH₂C(CH₃)₃ CH₂CH₃ 0 B-1096 H H F H H CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-1097 H H F H H CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-1098 H H F H H CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-1099 H H F H H CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-1100 H H F H H CH₂OCH₃ CH₂CH₃ 0 B-1101 H H F H H CH₂OCH₂CH₃ CH₂CH₃ 0 B-1102 H H F H H CH₂CH₂OCH₃ CH₂CH₃ 0 B-1103 H H F H H CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-1104 H H F H H CF₃ CH₂CH₃ 0 B-1105 H H F H H CHF₂ CH₂CH₃ 0 B-1106 H H F H H CH₂CF₃ CH₂CH₃ 0 B-1107 H H F H H CH₂CHF₂ CH₂CH₃ 0 B-1108 H H F H H CH₂CClF₂ CH₂CH₃ 0 B-1109 H H F H H CH₂CBrF₂ CH₂CH₃ 0 B-1110 H H F H H CF₂CF₃ CH₂CH₃ 0 B-1111 H H F H H CF₂CHF₂ CH₂CH₃ 0 B-1112 H H F H H CH₂CH₂CF₃ CH₂CH₃ 0 B-1113 H H F H H CH₂CF₂CF₃ CH₂CH₃ 0 B-1114 H H F H H CH₂CF₂CHF₂ CH₂CH₃ 0 B-1115 H H F H H CF₂CHFCF₃ CH₂CH₃ 0 B-1116 H H F H H CF₂CF₂CF₃ CH₂CH₃ 0 B-1117 H H F H H CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1118 H H F H H CH₂CF₂CFCF₃ CH₂CH₃ 0 B-1119 H H F H H CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1120 H H F H H CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-1121 H H F H H CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1122 H H F H H CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-1123 H H F H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1124 H H F H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1125 H H F H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1126 H H F H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-1127 H H F H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-1128 H H F H H CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1129 H H F H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1130 H H F H H CF₂CHFOCH₃ CH₂CH₃ 0 B-1131 H H F H H CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-1132 H H F H H CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-1133 H H F H H CF₂CHFOCF₃ CH₂CH₃ 0 B-1134 H H F H H CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-1135 H H F H H CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-1136 H H F H H CH₂CH═CH₂ CH₂CH₃ 0 B-1137 H H F H H CH₂CH═CHCl CH₂CH₃ 0 B-1138 H H F H H CH₂CH═CCl₂ CH₂CH₃ 0 B-1139 H H F H H CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-1140 H H F H H CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-1141 H H F H H CH₂C≡CH CH₂CH₃ 0 B-1142 H H F H H CH₂C≡CCH₃ CH₂CH₃ 0 B-1143 H H F H H CH₂C≡CI CH₂CH₃ 0 B-1144 H H F H H CH₂C≡CCF₃ CH₂CH₃ 0 B-1145 H H F H H cyclobutyl CH₂CH₃ 0 B-1146 H H F H H cyclopentyl CH₂CH₃ 0 B-1147 H H F H H cyclohexyl CH₂CH₃ 0 B-1148 H H F H H 4,4-difluorocyclohexyl CH₂CH₃ 0 B-1149 H H F H H CH₂(cyclopropyl) CH₂CH₃ 0 B-1150 H H F H H CH₂(cyclobutyl) CH₂CH₃ 0 B-1151 H H F H H CH₂(cyclopentyl) CH₂CH₃ 0 B-1152 H H F H H CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-1153 H H F H H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-1154 H H F H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0

TABLE 113 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1155 H H F H H CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-1156 H H F H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-1157 H H F H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-1158 H H F H H CH₂SCH₃ CH₂CH₃ 0 B-1159 H H F H H CH₂SCH₂CH₃ CH₂CH₃ 0 B-1160 H H F H H CH₂CH₂SCH₃ CH₂CH₃ 0 B-1161 H H F H H CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1162 H H F H H CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-1163 H H F H H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1164 H H F H H CH(CH₃)SCH₃ CH₂CH₃ 0 B-1165 H H F H H CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1166 H H F H H CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-1167 H H F H H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1168 H H F H H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-1169 H H F H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1170 H H F H H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-1171 H H F H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-1172 H H F H H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-1173 H H F H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1174 H H F H H CH₂SOCH₃ CH₂CH₃ 0 B-1175 H H F H H CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1176 H H F H H CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1177 H H F H H CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1178 H H F H H CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1179 H H F H H CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1180 H H F H H CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-1181 H H F H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1182 H H F H H CH₂SO₂CH₃ CH₂CH₃ 0 B-1183 H H F H H CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1184 H H F H H CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1185 H H F H H CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1186 H H F H H CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1187 H H F H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1188 H H F H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-1189 H H F H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1190 H H F H H CH₂SCF₃ CH₂CH₃ 0 B-1191 H H F H H CH₂SCHF₂ CH₂CH₃ 0 B-1192 H H F H H CH₂SCH₂CF₃ CH₂CH₃ 0 B-1193 H H F H H CH₂SCH₂CHF₂ CH₂CH₃ 0 B-1194 H H F H H CH₂SCF₂CF₃ CH₂CH₃ 0 B-1195 H H F H H CH₂CH₂SCF₃ CH₂CH₃ 0 B-1196 H H F H H CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1197 H H F H H CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-1198 H H F H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1199 H H F H H CH(CH₃)SCF₃ CH₂CH₃ 0 B-1200 H H F H H CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1201 H H F H H CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-1202 H H F H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1203 H H F H H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-1204 H H F H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1205 H H F H H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-1206 H H F H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-1207 H H F H H CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-1208 H H F H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1209 H H F H H CH₂SOCF₃ CH₂CH₃ 0 B-1210 H H F H H CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1211 H H F H H CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1212 H H F H H CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1213 H H F H H CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1214 H H F H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1215 H H F H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0

TABLE 114 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1216 H H F H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1217 H H F H H CH₂SO₂CF₃ CH₂CH₃ 0 B-1218 H H F H H CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1219 H H F H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1220 H H F H H CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1221 H H F H H CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1222 H H F H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1223 H H F H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-1224 H H F H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1225 H H F H H CH₂C(═O)CH₃ CH₂CH₃ 0 B-1226 H H F H H CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-1227 H H F H H CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-1228 H H F H H CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-1229 H H F H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-1230 H H F H H CH₂C(═O)CF₃ CH₂CH₃ 0 B-1231 H H F H H CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-1232 H H F H H CH₂C(═O)OCH₃ CH₂CH₃ 0 B-1233 H H F H H CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-1234 H H F H H CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-1235 H H F H H CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-1236 H H F H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-1237 H H F H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-1238 H H F H H CH₂C(═O)NH₂ CH₂CH₃ 0 B-1239 H H F H H CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-1240 H H F H H CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-1241 H H F H H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-1242 H H F H H CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-1243 H H F H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-1244 H H F H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-1245 H H F H H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-1246 H H F H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-1247 H H F H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-1248 H H F H H CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-1249 H H F H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-1250 H H F H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-1251 H H F H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-1252 H H F H H CH₂CH₂CH CH₂CH₃ 0 B-1253 H H F H H CH₂CH(OH)CH₃ CH₂CH₃ 0 B-1254 H H F H H CH₂CH₂CH₂OH CH₂CH₃ 0 B-1255 H H F H H CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-1256 H H F H H CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-1257 H H F H H CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0 B-1258 H H F H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-1259 H H F H H CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-1260 H H F H H CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-1261 H H F H H CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-1262 H H F H H CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-1263 H H F H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-1264 H H F H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-1265 H H F H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-1266 H H F H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-1267 H H F H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-1268 H H F H H CH₂Ph CH₂CH₃ 0 B-1269 H H F H H CH₂(2-F)Ph CH₂CH₃ 0 B-1270 H H F H H CH₂(3-F)Ph CH₂CH₃ 0 B-1271 H H F H H CH₂(4-F)Ph CH₂CH₃ 0 B-1272 H H F H H CH₂(2-Cl)Ph CH₂CH₃ 0 B-1273 H H F H H CH₂(3-Cl)Ph CH₂CH₃ 0 B-1274 H H F H H CH₂(4-Cl)Ph CH₂CH₃ 0 B-1275 H H F H H CH₂(2-CF₃)Ph CH₂CH₃ 0 B-1276 H H F H H CH₂(3-CF₃)Ph CH₂CH₃ 0

TABLE 115 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1277 H H F H H CH₂(4-CF₃)Ph CH₂CH₃ 0 B-1278 H H F H H CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-1279 H H F H H CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-1280 H H F H H CH₂CH₂Ph CH₂CH₃ 0 B-1281 Cl H H H H H H 0 B-1282 Cl H H H H CH₃ H 0 B-1283 Cl H H H H CH₂CH₃ H 0 B-1284 Cl H H H H CH(CH₃)₂ H 0 B-1285 Cl H H H H CH₂CH₂CH₃ H 0 B-1286 Cl H H H H CH₂CH(CH₃)₂ H 0 B-1287 Cl H H H H CH₂C(CH₃)₃ H 0 B-1288 Cl H H H H CH(CH₃)CH₂CH₃ H 0 B-1289 Cl H H H H CH₂(CH₂)₂CH₃ H 0 B-1290 Cl H H H H CH₂(CH₂)₃CH₃ H 0 B-1291 Cl H H H H CH₂(CH₂)₄CH₃ H 0 B-1292 Cl H H H H CH₂(CH₂)₆CH₃ H 0 B-1293 Cl H H H H CH₂OCH₃ H 0 B-1294 Cl H H H H CH₂OCH₂CH₃ H 0 B-1295 Cl H H H H CH₂CH₂OCH₃ H 0 B-1296 Cl H H H H CH₂CH₂OCH₂CH₃ H 0 B-1297 Cl H H H H CF₃ H 0 B-1298 Cl H H H H CHF₂ H 0 B-1299 Cl H H H H CH₂CF₃ H 0 B-1300 Cl H H H H CH₂CHF₂ H 0 B-1301 Cl H H H H CH₂CClF₂ H 0 B-1302 Cl H H H H CH₂CBrF₂ H 0 B-1303 Cl H H H H CF₂CF₃ H 0 B-1304 Cl H H H H CF₂CHF₂ H 0 B-1305 Cl H H H H CH₂CH₂CF₃ H 0 B-1306 Cl H H H H CH₂CF₂CF₃ H 0 B-1307 Cl H H H H CH₂CF₂CHF₂ H 0 B-1308 Cl H H H H CF₂CHFCF₃ H 0 B-1309 Cl H H H H CF₂CF₂CF₃ H 0 B-1310 Cl H H H H CH₂CF₂CF₂CF₃ H 0 B-1311 Cl H H H H CH₂CF₂CHFCF₃ H 0 B-1312 Cl H H H H CH₂CH₂CH₂CF₃ H 0 B-1313 Cl H H H H CH₂CH₂CF₂CF₃ H 0 B-1314 Cl H H H H CF₂CF₂CF₂CF₃ H 0 B-1315 Cl H H H H CH₂CH₂CH(CF₃)₂ H 0 B-1316 Cl H H H H CF₂CF₂CF₂CF₂CF₃ H 0 B-1317 Cl H H H H CH₂CF₂CF₂CF₂CF₃ H 0 B-1318 Cl H H H H CH₂CH₂CH₂CH₂CF₃ H 0 B-1319 Cl H H H H CH₂CF₂CF₂CF₂CHF₂ H 0 B-1320 Cl H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-1321 Cl H H H H CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-1322 Cl H H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-1323 Cl H H H H CF₂CHFOCH₃ H 0 B-1324 Cl H H H H CF₂CHFOCH₂CH₃ H 0 B-1325 Cl H H H H CH₂CH₂OCH₂CF₃ H 0 B-1326 Cl H H H H CF₂CHFOCF₃ H 0 B-1327 Cl H H H H CF₂CHFOCF₂CF₃ H 0 B-1328 Cl H H H H CF₂CHFOCF₂CF₂CF₃ H 0 B-1329 Cl H H H H CH₂CH═CH₂ H 0 B-1330 Cl H H H H CH₂CH═CHCl H 0 B-1331 Cl H H H H CH₂CH═CCl₂ H 0 B-1332 Cl H H H H CH₂CH₂CF═CF₂ H 0 B-1333 Cl H H H H CH₂CH₂CH═CF₂ H 0 B-1334 Cl H H H H CH₂C≡CH H 0 B-1335 Cl H H H H CH₂C≡CCH₃ H 0 B-1336 Cl H H H H CH₂C≡CI H 0 B-1337 Cl H H H H CH₂C≡CCF₃ H 0

TABLE 116 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1338 Cl H H H H cyclobutyl H 0 B-1339 Cl H H H H cyclopentyl H 0 B-1340 Cl H H H H cyclohexyl H 0 B-1341 Cl H H H H 4,4-difluorocyclohexyl H 0 B-1342 Cl H H H H CH₂(cyclopropyl) H 0 B-1343 Cl H H H H CH₂(cyclobutyl) H 0 B-1344 Cl H H H H CH₂(cyclopentyl) H 0 B-1345 Cl H H H H CH₂CH₂(cyclopropyl) H 0 B-1346 Cl H H H H CH₂(2,2-difluorocyclopropyl) H 0 B-1347 Cl H H H H CH₂(2,2-dichlorocyclopropyl) H 0 B-1348 Cl H H H H CH₂(4,4-difluorocyclohexyl) H 0 B-1349 Cl H H H H CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-1350 Cl H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-1351 Cl H H H H CH₂SCH₃ H 0 B-1352 Cl H H H H CH₂SCH₂CH₃ H 0 B-1353 Cl H H H H CH₂CH₂SCH₃ H 0 B-1354 Cl H H H H CH₂CH₂SCH₂CH₃ H 0 B-1355 Cl H H H H CH₂CH₂CH₂SCH₃ H 0 B-1356 Cl H H H H CH₂CH₂CH₂SCH₂CH₃ H 0 B-1357 Cl H H H H CH(CH₃)SCH₃ H 0 B-1358 Cl H H H H CH(CH₃)SCH₂CH₃ H 0 B-1359 Cl H H H H CH₂CH(CH₃)SCH₃ H 0 B-1360 Cl H H H H CH₂CH(CH₃)SCH₂CH₃ H 0 B-1361 Cl H H H H CH(CH₃)CH₂CH₂SCH₃ H 0 B-1362 Cl H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-1363 Cl H H H H CH₂CH(CH₃)CH₂SCH₃ H 0 B-1364 Cl H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-1365 Cl H H H H CH₂CH₂CH(CH₃)SCH₃ H 0 B-1366 Cl H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-1367 Cl H H H H CH₂SOCH₃ H 0 B-1368 Cl H H H H CH₂CH₂SOCH₃ H 0 B-1369 Cl H H H H CH₂CH₂CH₂SOCH₃ H 0 B-1370 Cl H H H H CH(CH₃)SOCH₃ H 0 B-1371 Cl H H H H CH₂CH(CH₃)SOCH₃ H 0 B-1372 Cl H H H H CH(CH₃)CH₂CH₂SOCH₃ H 0 B-1373 Cl H H H H CH₂CH(CH₃)CH₂SOCH₃ H 0 B-1374 Cl H H H H CH₂CH₂CH(CH₃)SOCH₃ H 0 B-1375 Cl H H H H CH₂SO₂CH₃ H 0 B-1376 Cl H H H H CH₂CH₂SO₂CH₃ H 0 B-1377 Cl H H H H CH₂CH₂CH₂SO₂CH₃ H 0 B-1378 Cl H H H H CH(CH₃)SO₂CH₃ H 0 B-1379 Cl H H H H CH₂CH(CH₃)SO₂CH₃ H 0 B-1380 Cl H H H H CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-1381 Cl H H H H CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-1382 Cl H H H H CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-1383 Cl H H H H CH₂SCF₃ H 0 B-1384 Cl H H H H CH₂SCHF₂ H 0 B-1385 Cl H H H H CH₂SCH₂CF₃ H 0 B-1386 Cl H H H H CH₂SCH₂CHF₂ H 0 B-1387 Cl H H H H CH₂SCF₂CF₃ H 0 B-1388 Cl H H H H CH₂CH₂SCF₃ H 0 B-1389 Cl H H H H CH₂CH₂SCH₂CF₃ H 0 B-1390 Cl H H H H CH₂CH₂CH₂SCF₃ H 0 B-1391 Cl H H H H CH₂CH₂CH₂SCH₂CF₃ H 0 B-1392 Cl H H H H CH(CH₃)SCF₃ H 0 B-1393 Cl H H H H CH(CH₃)SCH₂CF₃ H 0 B-1394 Cl H H H H CH₂CH(CH₃)SCF₃ H 0 B-1395 Cl H H H H CH₂CH(CH₃)SCH₂CF₃ H 0 B-1396 Cl H H H H CH(CH₃)CH₂CH₂SCF₃ H 0 B-1397 Cl H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-1398 Cl H H H H CH₂CH(CH₃)CH₂SCF₃ H 0

TABLE 117 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1399 Cl H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-1400 Cl H H H H CH₂CH₂CH(CH₃)SCF₃ H 0 B-1401 Cl H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-1402 Cl H H H H CH₂SOCF₃ H 0 B-1403 Cl H H H H CH₂CH₂SOCF₃ H 0 B-1404 Cl H H H H CH₂CH₂CH₂SOCF₃ H 0 B-1405 Cl H H H H CH(CH₃)SOCF₃ H 0 B-1406 Cl H H H H CH₂CH(CH₃)SOCF₃ H 0 B-1407 Cl H H H H CH(CH₃)CH₂CH₂SOCF₃ H 0 B-1408 Cl H H H H CH₂CH(CH₃)CH₂SOCF₃ H 0 B-1409 Cl H H H H CH₂CH₂CH(CH₃)SOCF₃ H 0 B-1410 Cl H H H H CH₂SO₂CF₃ H 0 B-1411 Cl H H H H CH₂CH₂SO₂CF₃ H 0 B-1412 Cl H H H H CH₂CH₂CH₂SO₂CF₃ H 0 B-1413 Cl H H H H CH(CH₃)SO₂CF₃ H 0 B-1414 Cl H H H H CH₂CH(CH₃)SO₂CF₃ H 0 B-1415 Cl H H H H CH(CH₃)CH₂CH₃SO₂CF₃ H 0 B-1416 Cl H H H H CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-1417 Cl H H H H CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-1418 Cl H H H H CH₂C(═O)CH₃ H 0 B-1419 Cl H H H H CH₂C(═O)CH₂CH₃ H 0 B-1420 Cl H H H H CH₂C(═O)C(CH₃)₃ H 0 B-1421 Cl H H H H CH₂CH₂C(═O)CH₃ H 0 B-1422 Cl H H H H CH₂CH₂C(═O)C(CH₃)₃ H 0 B-1423 Cl H H H H CH₂C(═O)CF₃ H 0 B-1424 Cl H H H H CH₂CH₂C(═O)CF₃ H 0 B-1425 Cl H H H H CH₂C(═O)OCH₃ H 0 B-1426 Cl H H H H CH₂C(═O)OCH₂CH₃ H 0 B-1427 Cl H H H H CH₂C(═O)OC(CH₃)₃ H 0 B-1428 Cl H H H H CH₂CH₂C(═O)OCH₃ H 0 B-1429 Cl H H H H CH₂CH₂C(═O)OCH₂CH₃ H 0 B-1430 Cl H H H H CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-1431 Cl H H H H CH₂C(═O)NH₂ H 0 B-1432 Cl H H H H CH₂CH₂C(═O)NH₂ H 0 B-1433 Cl H H H H CH₂C(═O)NHCH₃ H 0 B-1434 Cl H H H H CH₂C(═O)NHCH(CH₃)₂ H 0 B-1435 Cl H H H H CH₂CH₂C(═O)NHCH₃ H 0 B-1436 Cl H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-1437 Cl H H H H CH₂C(═O)NHCH₂CHF₂ H 0 B-1438 Cl H H H H CH₂C(═O)NHCH₂CF₃ H 0 B-1439 Cl H H H H CH₂CH₂C(═O)NHCH₂CHF₂ H 0 B-1440 Cl H H H H CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-1441 Cl H H H H CH₂C(═O)N(CH₃)₂ H 0 B-1442 Cl H H H H CH₂C(═O)N(CH₂CH₃)₂ H 0 B-1443 Cl H H H H CH₂CH₂C(═O)N(CH₃)₂ H 0 B-1444 Cl H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-1445 Cl H H H H CH₂CH₂OH H 0 B-1446 Cl H H H H CH₂CH(OH)CH₃ H 0 B-1447 Cl H H H H CH₂CH₂CH₂OH H 0 B-1448 Cl H H H H CH₂CH(OH)CH₂CH₃ H 0 B-1449 Cl H H H H CH₂CH(OH)C(CH₃)₃ H 0 B-1450 Cl H H H H CH₂CH₂CH(OH)CH₃ H 0 B-1451 Cl H H H H CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-1452 Cl H H H H CH₂C(═NOH)CH₃ H 0 B-1453 Cl H H H H CH₂C(═NOH)CH₂CH₃ H 0 B-1454 Cl H H H H CH₂C(═NOH)C(CH₃)₃ H 0 B-1455 Cl H H H H CH₂C(═NOCH₃)CH₃ H 0 B-1456 Cl H H H H CH₂C(═NOCH₃)CH₂CH₃ H 0 B-1457 Cl H H H H CH₂C(═NOCH₂CH₃)CH₃ H 0 B-1458 Cl H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-1459 Cl H H H H CH₂C(═NOCH₂CF₃)CH₃ H 0

TABLE 118 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1460 Cl H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0 B-1461 Cl H H H H CH₂Ph H 0 B-1462 Cl H H H H CH₂(2-F)Ph H 0 B-1463 Cl H H H H CH₂(3-F)Ph H 0 B-1464 Cl H H H H CH₂(4-F)Ph H 0 B-1465 Cl H H H H CH₂(2-Cl)Ph H 0 B-1466 Cl H H H H CH₂(3-Cl)Ph H 0 B-1467 Cl H H H H CH₂(4-Cl)Ph H 0 B-1468 Cl H H H H CH₂(2-CF₃)Ph H 0 B-1469 Cl H H H H CH₂(3-CF₃)Ph H 0 B-1470 Cl H H H H CH₂(4-CF₃)Ph H 0 B-1471 Cl H H H H CH₂(naphthalen-1-yl) H 0 B-1472 Cl H H H H CH₂(naphthalen-2-yl) H 0 B-1473 Cl H H H H CH₂CH₂Ph H 0 B-1474 Cl H H H H H CH₂CH₃ 0 B-1475 Cl H H H H CH₃ CH₂CH₃ 0 B-1476 Cl H H H H CH₂CH₃ CH₂CH₃ 0 B-1477 Cl H H H H CH(CH₃)₂ CH₂CH₃ 0 B-1478 Cl H H H H CH₂CH₂CH₃ CH₂CH₃ 0 B-1479 Cl H H H H CH₂CH(CH₃)₂ CH₂CH₃ 0 B-1480 Cl H H H H CH₂C(CH₃)₃ CH₂CH₃ 0 B-1481 Cl H H H H CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-1482 Cl H H H H CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-1483 Cl H H H H CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-1484 Cl H H H H CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-1485 Cl H H H H CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-1486 Cl H H H H CH₂OCH₃ CH₂CH₃ 0 B-1487 Cl H H H H CH₂OCH₂CH₃ CH₂CH₃ 0 B-1488 Cl H H H H CH₂CH₂OCH₃ CH₂CH₃ 0 B-1489 Cl H H H H CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-1490 Cl H H H H CF₃ CH₂CH₃ 0 B-1491 Cl H H H H CHF₂ CH₂CH₃ 0 B-1492 Cl H H H H CH₂CF₃ CH₂CH₃ 0 B-1493 Cl H H H H CH₂CHF₂ CH₂CH₃ 0 B-1494 Cl H H H H CH₂CClF₂ CH₂CH₃ 0 B-1495 Cl H H H H CH₂CBrF₂ CH₂CH₃ 0 B-1496 Cl H H H H CF₂CF₃ CH₂CH₃ 0 B-1497 Cl H H H H CF₂CHF₂ CH₂CH₃ 0 B-1498 Cl H H H H CH₂CH₂CF₃ CH₂CH₃ 0 B-1499 Cl H H H H CH₂CF₂CF₃ CH₂CH₃ 0 B-1500 Cl H H H H CH₂CF₂CHF₂ CH₂CH₃ 0 B-1501 Cl H H H H CF₂CHFCF₃ CH₂CH₃ 0 B-1502 Cl H H H H CF₂CF₂CF₃ CH₂CH₃ 0 B-1503 Cl H H H H CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1504 Cl H H H H CH₂CF₂CHFCF3 CH₂CH₃ 0 B-1505 Cl H H H H CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1506 Cl H H H H CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-1507 Cl H H H H CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1508 Cl H H H H CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-1509 Cl H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1510 Cl H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1511 Cl H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1512 Cl H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-1513 Cl H H H H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-1514 Cl H H H H CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1515 Cl H H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1516 Cl H H H H CF₂CHFOCH₃ CH₂CH₃ 0 B-1517 Cl H H H H CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-1518 Cl H H H H CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-1519 Cl H H H H CF₂CHFOCF₃ CH₂CH₃ 0 B-1520 Cl H H H H CF₂CHFOCF₂CF₃ CH₂CH₃ 0

TABLE 119 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1521 Cl H H H H CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-1522 Cl H H H H CH₂CH═CH₂ CH₂CH₃ 0 B-1523 Cl H H H H CH₂CH═CHCl CH₂CH₃ 0 B-1524 Cl H H H H CH₂CH═CCl₂ CH₂CH₃ 0 B-1525 Cl H H H H CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-1526 Cl H H H H CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-1527 Cl H H H H CH₂C≡CH CH₂CH₃ 0 B-1528 Cl H H H H CH₂C≡CCH₃ CH₂CH₃ 0 B-1529 Cl H H H H CH₂C≡CI CH₂CH₃ 0 B-1530 Cl H H H H CH₂C≡CCF₃ CH₂CH₃ 0 B-1531 Cl H H H H cyclobutyl CH₂CH₃ 0 B-1532 Cl H H H H cyclopentyl CH₂CH₃ 0 B-1533 Cl H H H H cyclohexyl CH₂CH₃ 0 B-1534 Cl H H H H 4,4-difluorocyclohexyl CH₂CH₃ 0 B-1535 Cl H H H H CH₂(cyclopropyl) CH₂CH₃ 0 B-1536 Cl H H H H CH₂(cyclobutyl) CH₂CH₃ 0 B-1537 Cl H H H H CH₂(cyclopentyl) CH₂CH₃ 0 B-1538 Cl H H H H CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-1539 Cl H H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-1540 Cl H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-1541 Cl H H H H CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-1542 Cl H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-1543 Cl H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-1544 Cl H H H H CH₂SCH₃ CH₂CH₃ 0 B-1545 Cl H H H H CH₂SCH₂CH₃ CH₂CH₃ 0 B-1546 Cl H H H H CH₂CH₂SCH₃ CH₂CH₃ 0 B-1547 Cl H H H H CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1548 Cl H H H H CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-1549 Cl H H H H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1550 Cl H H H H CH(CH₃)SCH₃ CH₂CH₃ 0 B-1551 Cl H H H H CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1552 Cl H H H H CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-1553 Cl H H H H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1554 Cl H H H H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-1555 Cl H H H H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1556 Cl H H H H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-1557 Cl H H H H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-1558 Cl H H H H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-1559 Cl H H H H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1560 Cl H H H H CH₂SOCH₃ CH₂CH₃ 0 B-1561 Cl H H H H CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1562 Cl H H H H CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1563 Cl H H H H CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1564 Cl H H H H CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1565 Cl H H H H CH(CH₃)CH₂CH₂SCCH₃ CH₂CH₃ 0 B-1566 Cl H H H H CH₂CH(CH₃)CH₂SCCH₃ CH₂CH₃ 0 B-1567 Cl H H H H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1568 Cl H H H H CH₂SO₂CH₃ CH₂CH₃ 0 B-1569 Cl H H H H CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1570 Cl H H H H CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1571 Cl H H H H CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1572 Cl H H H H CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1573 Cl H H H H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1574 Cl H H H H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-1575 Cl H H H H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1576 Cl H H H H CH₂SCF₃ CH₂CH₃ 0 B-1577 Cl H H H H CH₂SCHF₂ CH₂CH₃ 0 B-1578 Cl H H H H CH₂SCH₂CF₃ CH₂CH₃ 0 B-1579 Cl H H H H CH₂SCH₂CHF₂ CH₂CH₃ 0 B-1580 Cl H H H H CH₂SCF₂CF₃ CH₂CH₃ 0 B-1581 Cl H H H H CH₂CH₂SCF₃ CH₂CH₃ 0

TABLE 120 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1582 Cl H H H H CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1583 Cl H H H H CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-1584 Cl H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1585 Cl H H H H CH(CH₃)SCF₃ CH₂CH₃ 0 B-1586 Cl H H H H CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1587 Cl H H H H CH₂CH(CH₃)SCF₃ CH₂CH₂ 0 B-1588 Cl H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1589 Cl H H H H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-1590 Cl H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1591 Cl H H H H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-1592 Cl H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-1593 Cl H H H H CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-1594 Cl H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1595 Cl H H H H CH₂SOCF₃ CH₂CH₃ 0 B-1596 Cl H H H H CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1597 Cl H H H H CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1598 Cl H H H H CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1599 Cl H H H H CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1600 Cl H H H H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1601 Cl H H H H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-1602 Cl H H H H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1603 Cl H H H H CH₂SO₂CF₃ CH₂CH₃ 0 B-1604 Cl H H H H CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1605 Cl H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1606 Cl H H H H CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1607 Cl H H H H CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1608 Cl H H H H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1609 Cl H H H H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-1610 Cl H H H H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1611 Cl H H H H CH₂C(═O)CH₃ CH₂CH₃ 0 B-1612 Cl H H H H CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-1613 Cl H H H H CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-1614 Cl H H H H CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-1615 Cl H H H H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-1616 Cl H H H H CH₂C(═O)CF₃ CH₂CH₃ 0 B-1617 Cl H H H H CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-1618 Cl H H H H CH₂C(═O)OCH₃ CH₂CH₃ 0 B-1619 Cl H H H H CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-1620 Cl H H H H CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-1621 Cl H H H H CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-1622 Cl H H H H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-1623 Cl H H H H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-1624 Cl H H H H CH₂C(═O)NH₂ CH₂CH₃ 0 B-1625 Cl H H H H CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-1626 Cl H H H H CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-1627 Cl H H H H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-1628 Cl H H H H CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-1629 Cl H H H H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-1630 Cl H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-1631 Cl H H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-1632 Cl H H H H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-1633 Cl H H H H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-1634 Cl H H H H CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-1635 Cl H H H H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-1636 Cl H H H H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-1637 Cl H H H H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-1638 Cl H H H H CH₂CH₂OH CH₂CH₃ 0 B-1639 Cl H H H H CH₂CH(OH)CH₃ CH₂CH₃ 0 B-1640 Cl H H H H CH₂CH₂CH₂OH CH₂CH₃ 0 B-1641 Cl H H H H CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-1642 Cl H H H H CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0

TABLE 121 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1643 Cl H H H H CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0 B-1644 Cl H H H H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-1645 Cl H H H H CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-1646 Cl H H H H CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-1647 Cl H H H H CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-1648 Cl H H H H CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-1649 Cl H H H H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-1650 Cl H H H H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-1651 Cl H H H H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-1652 Cl H H H H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-1653 Cl H H H H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-1654 Cl H H H H CH₂Ph CH₂CH₃ 0 B-1555 Cl H H H H CH₂(2-F)Ph CH₂CH₃ 0 B-1656 Cl H H H H CH₂(3-F)Ph CH₂CH₃ 0 B-1657 Cl H H H H CH₂(4-F)Ph CH₂CH₃ 0 B-1658 Cl H H H H CH₂(2-Cl)Ph CH₂CH₃ 0 B-1659 Cl H H H H CH₂(3-Cl)Ph CH₂CH₃ 0 B-1560 Cl H H H H CH₂(4-Cl)Ph CH₂CH₃ 0 B-1661 Cl H H H H CH₂(2-CF₃)Ph CH₂CH₃ 0 B-1662 Cl H H H H CH₂(3-CF₃)Ph CH₂CH₃ 0 B-1663 Cl H H H H CH₂(4-CF₃)Ph CH₂CH₃ 0 B-1664 Cl H H H H CH₂(naphthalen-1-yl) CH₂CH₃ 0 B-1665 Cl H H H H CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-1666 Cl H H H H CH₂CH₂Ph CH₂CH₃ 0 B-1667 H H H Cl H H H 0 B-1668 H H H Cl H CH₃ H 0 B-1669 H H H Cl H CH₂CH₃ H 0 B-1670 H H H Cl H CH(CH₃)₂ H 0 B-1671 H H H Cl H CH₂CH₂CH₃ H 0 B-1672 H H H Cl H CH₂CH(CH₃)₂ H 0 B-1673 H H H Cl H CH₂C(CH₃)₃ H 0 B-1674 H H H Cl H CH(CH₃)CH₂CH₃ H 0 B-1675 H H H Cl H CH₂(CH₂)₂CH₃ H 0 B-1676 H H H Cl H CH₂(CH₂)₃CH₃ H 0 B-1677 H H H Cl H CH₂(CH₂)₄CH₃ H 0 B-1678 H H H Cl H CH₂(CH₂)₆CH₃ H 0 B-1679 H H H Cl H CH₂OCH₃ H 0 B-1680 H H H Cl H CH₂OCH₂CH₃ H 0 B-1681 H H H Cl H CH₂CH₂OCH₃ H 0 B-1682 H H H Cl H CH₂CH₂OCH₂CH₃ H 0 B-1683 H H H Cl H CF₃ H 0 B-1684 H H H Cl H CHF₂ H 0 B-1685 H H H Cl H CH₂CF₃ H 0 B-1686 H H H Cl H CH₂CHF₂ H 0 B-1687 H H H Cl H CH₂CClF₂ H 0 B-1688 H H H Cl H CH₂CBrF₂ H 0 B-1689 H H H Cl H CF₂CF₃ H 0 B-1690 H H H Cl H CF₂CHF₂ H 0 B-1691 H H H Cl H CH₂CH₂CF₃ H 0 B-1692 H H H Cl H CH₂CF₂CF₃ H 0 B-1693 H H H Cl H CH₂CF₂CHF₂ H 0 B-1694 H H H Cl H CF₂CHFCF₃ H 0 B-1695 H H H Cl H CF₂CF₂CF₃ H 0 B-1696 H H H Cl H CH₂CF₂CF₂CF₃ H 0 B-1697 H H H Cl H CH₂CF₂CHFCF₃ H 0 B-1698 H H H Cl H CH₂CH₂CH₂CF₃ H 0 B-1699 H H H Cl H CH₂CH₂CF₂CF₃ H 0 B-1700 H H H Cl H CF₂CF₂CF₂CF₃ H 0 B-1701 H H H Cl H CH₂CH₂CH(CF₃)₂ H 0 B-1702 H H H Cl H CF₂CF₂CF₂CF₂CF₃ H 0 B-1703 H H H Cl H CH₂CF₂CF₂CF₂CF₃ H 0

TABLE 122 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1704 H H H Cl H CH₂CH₂CH₂CH₂CF₃ H 0 B-1705 H H H Cl H CH₂CF₂CF₂CF₂CHF₂ H 0 B-1706 H H H Cl H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-1707 H H H Cl H CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-1708 H H H Cl H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-1709 H H H Cl H CF₂CHFOCH₃ H 0 B-1710 H H H Cl H CF₂CHOCH₂CH₃ H 0 B-1711 H H H Cl H CH₂CH₂OCH₂CF₃ H 0 B-1712 H H H Cl H CF₂CHFOCF₃ H 0 B-1713 H H H Cl H CF₂CHFCCF₂CF₃ H 0 B-1714 H H H Cl H CF₂CHFOCF₂CF₂CF₃ H 0 B-1715 H H H Cl H CH₂CH═CH₂ H 0 B-1716 H H H Cl H CH₂CH═CHCl H 0 B-1717 H H H Cl H CH₂CH═CCl₂ H 0 B-1718 H H H Cl H CH₂CH₂CF═CF₂ H 0 B-1719 H H H Cl H CH₂CH₃CH═CF₂ H 0 B-1720 H H H Cl H CH₂C≡CH H 0 B-1721 H H H Cl H CH₂C≡CCH₃ H 0 B-1722 H H H Cl H CH₂C≡Cl H 0 B-1723 H H H Cl H CH₂C≡CCF₃ H 0 B-1724 H H H Cl H cyclobutyl H 0 B-1725 H H H Cl H cyclopentyl H 0 B-1726 H H H Cl H cyclohexyl H 0 B-1727 H H H Cl H 4,4-difluorocyclohexyl H 0 B-1728 H H H Cl H CH₂(cyclopropyl) H 0 B-1729 H H H Cl H CH₂(cyclobutyl) H 0 B-1730 H H H Cl H CH₂(cyclopentyl) H 0 B-1731 H H H Cl H CH₂CH₂(cyclopropyl) H 0 B-1732 H H H Cl H CH₂(2,2-difluorocyclopropyl) H 0 B-1733 H H H Cl H CH₂(2,2-dichlorocyclopropyl) H 0 B-1734 H H H Cl H CH₂(4,4-difluorocyclohexyl) H 0 B-1735 H H H Cl H CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-1736 H H H Cl H CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-1737 H H H Cl H CH₂SCH₃ H 0 B-1738 H H H Cl H CH₂SCH₂CH₃ H 0 B-1739 H H H Cl H CH₂CH₂SCH₃ H 0 B-1740 H H H Cl H CH₂CH₂SCH₂CH₃ H 0 B-1741 H H H Cl H CH₂CH₂CH₂SCH₃ H 0 B-1742 H H H Cl H CH₂CH₂CH₂SCH₂CH₃ H 0 B-1743 H H H Cl H CH(CH₃)SCH₃ H 0 B-1744 H H H Cl H CH(CH₃)SCH₂CH₃ H 0 B-1745 H H H Cl H CH₂CH(CH₃)SCH₃ H 0 B-1746 H H H Cl H CH₂CH(CH₃)SCH₂CH₃ H 0 B-1747 H H H Cl H CH(CH₃)CH₂CH₂SCH₃ H 0 B-1748 H H H Cl H CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-1749 H H H Cl H CH₂CH(CH₃)CH₂SCH₃ H 0 B-1750 H H H Cl H CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-1751 H H H Cl H CH₂CH₂CH(CH₃)SCH₃ H 0 B-1752 H H H Cl H CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-1753 H H H Cl H CH₂SOCH₃ H 0 B-1754 H H H Cl H CH₂CH₂SOCH₃ H 0 B-1755 H H H Cl H CH₂CH₂CH₂SOCH₃ H 0 B-1756 H H H Cl H CH(CH₃)SOCH₃ H 0 B-1757 H H H Cl H CH₂CH(CH₃)SOCH₃ H 0 B-1758 H H H Cl H CH(CH₃)CH₂CH₂SOCH₃ H 0 B-1759 H H H Cl H CH₂CH(CH₃)CH₂SOCH₃ H 0 B-1760 H H H Cl H CH₂CH₂CH(CH₃)SOCH₃ H 0 B-1761 H H H Cl H CH₂SO₂CH₃ H 0 B-1762 H H H Cl H CH₂CH₂SO₂CH₃ H 0 B-1763 H H H Cl H CH₂CH₂CH₂SO₂CH₃ H 0 B-1764 H H H Cl H CH(CH₃)SO₂CH₃ H 0

TABLE 123 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1765 H H H Cl H CH₂CH(CH₃)SO₂CH₃ H 0 B-1766 H H H Cl H CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-1767 H H H Cl H CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-1768 H H H Cl H CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-1769 H H H Cl H CH₂SCF₃ H 0 B-1770 H H H Cl H CH₂SCHF₂ H 0 B-1771 H H H Cl H CH₂SCH₂CF₃ H 0 B-1772 H H H Cl H CH₂SCH₂CHF₂ H 0 B-1773 H H H Cl H CH₂SCF₂CF₃ H 0 B-1774 H H H Cl H CH₂CH₂SCF₃ H 0 B-1775 H H H Cl H CH₂CH₂SCH₂CF₃ H 0 B-1776 H H H Cl H CH₂CH₂CH₂SCF₃ H 0 B-1777 H H H Cl H CH₂CH₂CH₂SCH₂CF₃ H 0 B-1778 H H H Cl H CH(CH₃)SCF₃ H 0 B-1779 H H H Cl H CH(CH₃)SCH₂CF₃ H 0 B-1780 H H H Cl H CH₂CH(CH₃)SCF₃ H 0 B-1781 H H H Cl H CH₂CH(CH₃)SCH₂CF₃ H 0 B-1782 H H H Cl H CH(CH₃)CH₂CH₂SCF₃ H 0 B-1783 H H H Cl H CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-1784 H H H Cl H CH₂CH(CH₃)CH₂SCF₃ H 0 B-1785 H H H Cl H CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-1786 H H H Cl H CH₂CH₂CH(CH₃)SCF₃ H 0 B-1787 H H H Cl H CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-1788 H H H Cl H CH₂SOCF₃ H 0 B-1789 H H H Cl H CH₂CH₂SOCF₃ H 0 B-1790 H H H Cl H CH₂CH₂CH₂SOCF₃ H 0 B-1791 H H H Cl H CH(CH₃)SOCF₃ H 0 B-1792 H H H Cl H CH₂CH(CH₃)SOCF₃ H 0 B-1793 H H H Cl H CH(CH₃)CH₂CH₂SOCF₃ H 0 B-1794 H H H Cl H CH₂CH(CH₃)CH₂SOCF₃ H 0 B-1795 H H H Cl H CH₂CH₂CH(CH₃)SOCF₃ H 0 B-1796 H H H Cl H CH₂SO₂CF₃ H 0 B-1797 H H H Cl H CH₂CH₂SO₂CF₃ H 0 B-1798 H H H Cl H CH₂CH₂CH₂SO₂CF₃ H 0 B-1799 H H H Cl H CH(CH₃)SO₂CF₃ H 0 B-1800 H H H Cl H CH₂CH(CH₃)SO₂CF₃ H 0 B-1801 H H H Cl H CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-1802 H H H Cl H CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-1803 H H H Cl H CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-1804 H H H Cl H CH₂C(═O)CH₃ H 0 B-1805 H H H Cl H CH₂C(═O)CH₂CH₃ H 0 B-1806 H H H Cl H CH₂C(═O)C(CH₃)₃ H 0 B-1807 H H H Cl H CH₂CH₂C(═O)CH₃ H 0 B-1808 H H H Cl H CH₂CH₂C(═O)C(CH₃)₃ H 0 B-1809 H H H Cl H CH₂C(═O)CF₃ H 0 B-1810 H H H Cl H CH₂CH₂C(═O)CF₃ H 0 B-1811 H H H Cl H CH₂C(═O)OCH₃ H 0 B-1812 H H H Cl H CH₂C(═O)OCH₂CH₃ H 0 B-1813 H H H Cl H CH₂C(═O)OC(CH₃)₃ H 0 B-1814 H H H Cl H CH₂CH₂C(═O)OCH₃ H 0 B-1815 H H H Cl H CH₂CH₂C(═O)OCH₂CH₃ H 0 B-1816 H H H Cl H CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-1817 H H H Cl H CH₂C(═O)NH₂ H 0 B-1818 H H H Cl H CH₂CH₂C(═O)NH₂ H 0 B-1819 H H H Cl H CH₂C(═O)NHCH₃ H 0 B-1820 H H H Cl H CH₂C(═O)NHCH(CH₃)₂ H 0 B-1821 H H H Cl H CH₂CH₂C(═O)NHCH₃ H 0 B-1822 H H H Cl H CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-1823 H H H Cl H CH₂C(═O)NHCH₂CHF₂ H 0 B-1824 H H H Cl H CH₂C(═O)NHCH₂CF₃ H 0 B-1825 H H H Cl H CH₂CH₂C(═O)NHCH₂CHF₂ H 0

TABLE 124 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1826 H H H Cl H CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-1827 H H H Cl H CH₂C(═O)N(CH₃)₂ H 0 B-1828 H H H Cl H CH₂C(═O)N(CH₂CH₃)₂ H 0 B-1829 H H H Cl H CH₂CH₂C(═O)N(CH₃)₂ H 0 B-1830 H H H Cl H CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-1831 H H H Cl H CH₂CH₂OH H 0 B-1832 H H H Cl H CH₂CH(OH)CH₃ H 0 B-1833 H H H Cl H CH₂CH₂CH₂OH H 0 B-1834 H H H Cl H CH₂CH(OH)CH₂CH₃ H 0 B-1835 H H H Cl H CH₂CH(OH)C(CH₃)₃ H 0 B-1836 H H H Cl H CH₂CH₂CH(OH)CH₃ H 0 B-1837 H H H Cl H CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-1838 H H H Cl H CH₂C(═NOH)CH₃ H 0 B-1839 H H H Cl H CH₂C(═NOH)CH₂CH₃ H 0 B-1840 H H H Cl H CH₂C(═NOH)C(CH₃)₃ H 0 B-1841 H H H Cl H CH₂C(═NOCH₃)CH₃ H 0 B-1842 H H H Cl H CH₂C(═NOCH₃)CH₂CH₃ H 0 B-1843 H H H Cl H CH₂C(═NOCH₂CH₃)CH₃ H 0 B-1844 H H H Cl H CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-1845 H H H Cl H CH₂C(═NOCH₂CF₃)CH₃ H 0 B-1846 H H H Cl H CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0 B-1847 H H H Cl H CH₂Ph H 0 B-1848 H H H Cl H CH₂(2-F)Ph H 0 B-1849 H H H Cl H CH₂(3-F)Ph H 0 B-1850 H H H Cl H CH₂(4-F)Ph H 0 B-1851 H H H Cl H CH₂(2-Cl)Ph H 0 B-1852 H H H Cl H CH₂(3-Cl)Ph H 0 B-1853 H H H Cl H CH₂(4-Cl)Ph H 0 B-1854 H H H Cl H CH₂(2-CF₃)Ph H 0 B-1855 H H H Cl H CH₂(3-CF₃)Ph H 0 B-1856 H H H Cl H CH₂(4-CF₃)Ph H 0 B-1857 H H H Cl H CH₂(naphthalen-1-yl) H 0 B-1858 H H H Cl H CH₂(naphthalen-2-yl) H 0 B-1859 H H H Cl H CH₂CH₂Ph H 0 B-1860 H H H Cl H H CH₂CH₃ 0 B-1861 H H H Cl H CH₃ CH₂CH₃ 0 B-1862 H H H Cl H CH₂CH₃ CH₂CH₃ 0 B-1863 H H H Cl H CH(CH₃)₂ CH₂CH₃ 0 B-1864 H H H Cl H CH₂CH₂CH₃ CH₂CH₃ 0 B-1865 H H H Cl H CH₂CH(CH₃)₂ CH₂CH₃ 0 B-1866 H H H Cl H CH₂C(CH₃)₃ CH₂CH₃ 0 B-1867 H H H Cl H CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-1868 H H H Cl H CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-1869 H H H Cl H CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-1870 H H H Cl H CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-1871 H H H Cl H CH₂(CH₂)₆CH₃ CH₂CH₃ c B-1872 H H H Cl H CH₂OCH₃ CH₂CH₃ 0 B-1873 H H H Cl H CH₂OCH₂CH₃ CH₂CH₃ 0 B-1874 H H H Cl H CH₂CH₂OCH₃ CH₂CH₃ 0 B-1875 H H H Cl H CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-1876 H H H Cl H CF₃ CH₂CH₃ 0 B-1877 H H H Cl H CHF₂ CH₂CH₃ 0 B-1878 H H H Cl H CH₂CF₃ CH₂CH₃ 0 B-1879 H H H Cl H CH₂CHF₂ CH₂CH₃ 0 B-1880 H H H Cl H CH₂CClF₂ CH₂CH₃ 0 B-1881 H H H Cl H CH₂CBrF₂ CH₂CH₃ 0 B-1882 H H H Cl H CF₂CF₃ CH₂CH₃ 0 B-1883 H H H Cl H CF₂CHF₂ CH₂CH₃ 0 B-1884 H H H Cl H CH₂CH₂CF₃ CH₂CH₃ 0 B-1885 H H H Cl H CH₂CF₂CF₃ CH₂CH₃ 0 B-1886 H H H Cl H CH₂CF₂CHF₂ CH₂CH₃ 0

TABLE 125 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1887 H H H Cl H CF₂CHFCF₃ CH₂CH₃ 0 B-1888 H H H Cl H CF₂CF₂CF₃ CH₂CH₃ 0 B-1889 H H H Cl H CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1890 H H H Cl H CH₂CF₂CHFCF₃ CH₂CH₃ 0 B-1891 H H H Cl H CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1892 H H H Cl H CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-1893 H H H Cl H CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1894 H H H Cl H CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-1895 H H H Cl H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1896 H H H Cl H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-1897 H H H Cl H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1898 H H H Cl H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-1899 H H H Cl H CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-1900 H H H Cl H CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1901 H H H Cl H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-1902 H H H Cl H CF₂CHFOCH₃ CH₂CH₃ 0 B-1903 H H H Cl H CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-1904 H H H Cl H CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-1905 H H H Cl H CF₂CHFOCF₃ CH₂CH₃ 0 B-1906 H H H Cl H CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-1907 H H H Cl H CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-1908 H H H Cl H CH₂CH═CH₂ CH₂CH₃ 0 B-1909 H H H Cl H CH₂CH═CHCl CH₂CH₃ 0 B-1910 H H H Cl H CH₂CH═CCl₂ CH₂CH₃ 0 B-1911 H H H Cl H CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-1912 H H H Cl H CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-1913 H H H Cl H CH₂C≡CH CH₂CH₃ 0 B-1914 H H H Cl H CH₂C≡CCH₃ CH₂CH₃ 0 B-1915 H H H Cl H CH₂C≡Cl CH₂CH₃ 0 B-1916 H H H Cl H CH₂C≡CCF₃ CH₂CH₃ 0 B-1917 H H H Cl H cyclobutyl CH₂CH₃ 0 B-1918 H H H Cl H cyclopentyl CH₂CH₃ 0 B-1919 H H H Cl H cyclohexyl CH₂CH₃ 0 B-1920 H H H Cl H 4,4-difluorocyclohexyl CH₂CH₃ 0 B-1921 H H H Cl H CH₂(cyclopropyl) CH₂CH₃ 0 B-1922 H H H Cl H CH₂(cyclobutyl) CH₂CH₃ 0 B-1923 H H H Cl H CH₂(cyclopentyl) CH₂CH₃ 0 B-1924 H H H Cl H CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-1925 H H H Cl H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-1926 H H H Cl H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-1927 H H H Cl H CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-1928 H H H Cl H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-1929 H H H Cl H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-1930 H H H Cl H CH₂SCH₃ CH₂CH₃ 0 B-1931 H H H Cl H CH₂SCH₂CH₃ CH₂CH₃ 0 B-1932 H H H Cl H CH₂CH₂SCH₃ CH₂CH₃ 0 B-1933 H H H Cl H CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1934 H H H Cl H CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-1935 H H H CI H CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1936 H H H Cl H CH(CH₃)SCH₃ CH₂CH₃ 0 B-1937 H H H Cl H CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1938 H H H Cl H CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-1939 H H H Cl H CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1940 H H H Cl H CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-1941 H H H Cl H CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-1942 H H H Cl H CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-1943 H H H Cl H CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-1944 H H H Cl H CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-1945 H H H Cl H CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-1946 H H H Cl H CH₂SOCH₃ CH₂CH₃ 0 B-1947 H H H Cl H CH₂CH₂SOCH₃ CH₂CH₃ 0

TABLE 126 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-1948 H H H Cl H CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1949 H H H Cl H CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1950 H H H Cl H CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1951 H H H Cl H CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-1952 H H H Cl H CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-1953 H H H Cl H CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-1954 H H H Cl H CH₂SO₂CH₃ CH₂CH₃ 0 B-1955 H H H Cl H CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1956 H H H Cl H CH₂CH₂CH₂SO₂CH₃ CH₃CH₃ 0 B-1957 H H H Cl H CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1958 H H H Cl H CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1959 H H H Cl H CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-1960 H H H Cl H CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-1961 H H H Cl H CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-1962 H H H Cl H CH₂SCF₃ CH₂CH₃ 0 B-1963 H H H Cl H CH₂SCHF₂ CH₂CH₃ 0 B-1964 H H H Cl H CH₂SCH₂CF₃ CH₂CH₃ 0 B-1965 H H H Cl H CH₂SCH₂CHF₂ CH₂CH₃ 0 B-1966 H H H Cl H CH₂SCF₂CF₃ CH₂CH₃ 0 B-1967 H H H Cl H CH₂CH₂SCF₃ CH₂CH₃ 0 B-1968 H H H Cl H CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1969 H H H Cl H CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-1970 H H H Cl H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-1971 H H H Cl H CH(CH₃)SCF₃ CH₂CH₃ 0 B-1972 H H H Cl H CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1973 H H H Cl H CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-1974 H H H Cl H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1975 H H H Cl H CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-1976 H H H Cl H CH(CH₃)CH₂CH₂SCH₂CF₃ CB₂CH₃ 0 B-1977 H H H Cl H CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-1978 H H H Cl H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-1979 H H H Cl H CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-1980 H H H Cl H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-1981 H H H Cl H CH₂SOCF₃ CH₂CH₃ 0 B-1982 H H H Cl H CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1983 H H H Cl H CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1984 H H H Cl H CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1985 H H H Cl H CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1986 H H H Cl H CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-1987 H H H Cl H CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-1988 H H H Cl H CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-1989 H H H Cl H CH₂SO₂CF₃ CH₂CH₃ 0 B-1990 H H H Cl H CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1991 H H H Cl H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B 1992 H H H Cl H CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1993 H H H Cl H CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1994 H H H Cl H CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-1995 H H H Cl H CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-1996 H H H Cl H CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-1997 H H H Cl H CH₂C(═O)CH₃ CH₂CH₃ 0 B-1998 H H H Cl H CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-1999 H H H Cl H CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-2000 H H H Cl H CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-2001 H H H Cl H CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-2002 H H H Cl H CH₂C(═O)CF₃ CH₂CH₃ 0 B-2003 H H H Cl H CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-2004 H H H Cl H CH₂C(═O)OCH₃ CH₂CH₃ 0 B-2005 H H H Cl H CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-2006 H H H Cl H CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-2007 H H H Cl H CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-2008 H H H Cl H CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0

TABLE 127 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2009 H H H Cl H CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-2010 H H H Cl H CH₂C(═O)NH₂ CH₂CH₃ 0 B-2011 H H H Cl H CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-2012 H H H Cl H CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-2013 H H H Cl H CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-2014 H H H Cl H CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-2015 H H H Cl H CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-2016 H H H Cl H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-2012 H H H Cl H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-2018 H H H Cl H CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-2019 H H H Cl H CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-2020 H H H Cl H CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-2021 H H H Cl H CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-2022 H H H Cl H CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-2023 H H H Cl H CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-2024 H H H Cl H CH₂CH₂OH CH₂CH₃ 0 B-2025 H H H Cl H CH₂CH(OH)CH₃ CH₂CH₃ 0 B-2026 H H H Cl H CH₂CH₂CH₂OH CH₂CH₃ 0 B-2027 H H H Cl H CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-2028 H H H Cl H CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-2029 H H H Cl H CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0 B-2030 H H H Cl H CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-2031 H H H Cl H CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-2032 H H H Cl H CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-2033 H H H Cl H CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-2034 H H H Cl H CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-2035 H H H Cl H CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-2036 H H H Cl H CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-2037 H H H Cl H CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-2038 H H H Cl H CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-2039 H H H Cl H CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-2040 H H H Cl H CH₂Ph CH₂CH₃ 0 B-2041 H H H Cl H CH₂(2-F)Ph CH₂CH₃ 0 B-2042 H H H Cl H CH₂(3-F)Ph CH₂CH₃ 0 B-2043 H H H Cl H CH₂(4-F)Ph CH₂CH₃ 0 B-2044 H H H Cl H CH₂(2-Cl)Ph CH₂CH₃ 0 B-2045 H H H Cl H CH₂(3-CI)Ph CH₂CH₃ 0 B-2046 H H H Cl H CH₂(4-Cl)Ph CH₂CH₃ 0 B-2047 H H H Cl H CH₂(2-CF₃)Ph CH₂CH₃ 0 B-2048 H H H Cl H CH₂(3-CF₃)Ph CH₂CH₃ 0 B-2049 H H H Cl H CH₂(4-CF₃)Ph CH₂CH₃ 0 B-2050 H H H Cl H CH₂(naphthalen-1-yl) CH₂CH₃ 0 B-2051 H H H Cl H CH₂(naphtbalen-2-yl) CH₂CH₃ 0 B-2052 H H H Cl H CH₂CH₂Ph CH₂CH₃ 0 B-2053 H H H H Cl H H 0 B-2054 H H H H Cl CH₃ H 0 B-2055 H H H H Cl CH₂CH₃ H 0 B-2056 H H H H Cl CH(CH₃)₂ H 0 B-2057 H H H H Cl CH₂CH₂CH₃ H 0 B-2058 H H H H Cl CH₂CH(CH₃)₂ H 0 B-2059 H H H H Cl CH₂C(CH₃)₃ H 0 B-2060 H H H H Cl CH(CH₃)CH₂CH₃ H 0 B-2061 H H H H Cl CH₂(CH₂)₂CH₃ H 0 B-2062 H H H H Cl CH₂(CH₂)₃CH₃ H 0 B-2063 H H H H Cl CH₂(CH₂)₄CH₃ H 0 B-2064 H H H H Cl CH₂(CH₂)₆CH₃ H 0 B-2065 H H H H Cl CH₂OCH₃ H 0 B-2066 H H H H Cl CH₂OCH₂CH₃ H 0 B-2067 H H H H Cl CH₂CH₂OCH₃ H 0 B-2068 H H H H Cl CH₂CH₂OCH₂CH₃ H 0 B-2069 H H H H Cl CF₃ H 0

TABLE 128 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2070 H H H H Cl CHF₂ H 0 B-2071 H H H H Cl CH₂CF₃ H 0 B-2072 H H H H Cl CH₂CHF₂ H 0 B-2073 H H H H Cl CH₃CClF₂ H 0 B-2074 H H H H Cl CH₂CBrF₂ H 0 B-2075 H H H H Cl CF₂CF₃ H 0 B-2076 H H H H Cl CF₂CHF₂ H 0 B-2077 H H H H Cl CH₂CH₂CF₃ H 0 B-2078 H H H H Cl CH₂CF₂CF₃ H 0 B-2079 H H H H Cl CH₂CF₂CHF₂ H 0 B-2080 H H H H Cl CF₂CHFCF₃ H 0 B-2081 H H H H Cl CF₂CF₂CF₃ H 0 B-2082 H H H H Cl CH₂CF₂CF₂CF₃ H 0 B-2083 H H H H Cl CH₂CF₂CHFCF₃ H 0 B-2084 H H H H Cl CH₂CH₂CH₂CF₃ H 0 B-2085 H H H H Cl CH₂CH₂CF₂CF₃ H 0 B-2086 H H H H Cl CF₂CF₂CF₂CF₃ H 0 B-2087 H H H H Cl CH₂CH₂CH(CF₃)₂ H 0 B-2088 H H H H Cl CF₂CF₂CF₂CF₂CF₃ H 0 B-2089 H H H H Cl CH₂CF₂CF₂CF₂CF₃ H 0 B-2090 H H H H Cl CH₂CH₂CH₂CH₂CF₃ H 0 B-2091 H H H H Cl CH₂CF₃CF₂CF₂CHF₂ H 0 B-2092 H H H H Cl CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-2093 H H H H Cl CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-2094 H H H H Cl CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-2095 H H H H Cl CF₂CHFOCH₃ H 0 B-2096 H H H H Cl CF₂CHFOCH₂CH₃ H 0 B-2097 H H H H Cl CH₂CH₂OCH₂CF₃ H 0 B-2098 H H H H Cl CF₂CHFOCF₃ H 0 B-2099 H H H H Cl CF₂CHFOCF₂CF₃ H 0 B-2100 H H H H Cl CF₂CHFOCF₂CF₂CF₃ H 0 B-2101 H H H H Cl CH₂CH═CH₂ H 0 B-2102 H H H H Cl CH₂CH═CHCl H 0 B-2103 H H H H Cl CH₂CH═CCl₂ H 0 B-2104 H H H H Cl CH₂CH₂CF═CF₂ H 0 B-2105 H H H H Cl CH₂CH₂CH═CF₂ H 0 B-2106 H H H H Cl CH₂C≡CH H 0 B-2107 H H H H Cl CH₂C≡CCH₃ H 0 B-2108 H H H H Cl CH₂C≡Cl H 0 B-2109 H H H H Cl CH₂C≡CCF₃ H 0 B-2110 H H H H Cl cyclobutyl H 0 B-2111 H H H H Cl cyclopentyl H 0 B-2112 H H H H Cl cyclohexyl H 0 B-2113 H H H H Cl 4,4-difluorocyclohexyl H 0 B-2114 H H H H Cl CH₂(cyclopropyl) H 0 B-2115 H H H H Cl CH₂(cyclobutyl) H 0 B-2116 H H H H Cl CH₂(cyclopentyl) H 0 B-2117 H H H H Cl CH₂CH₂(cyclopropyl) H 0 B-2118 H H H H Cl CH₂(2,2-difluorocyclopropyl) H 0 B-2119 H H H H Cl CH₂(2,2-dichlorocyclopropyl) H 0 B-2120 H H H H Cl CH₂(4,4-difluorocyclohexyl) H 0 B-2121 H H H H Cl CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-2122 H H H H Cl CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-2123 H H H H Cl CH₂SCH₃ H 0 B-2124 H H H H Cl CH₂SCH₂CH₃ H 0 B-2125 H H H H Cl CH₂CH₂SCH₃ H 0 B-2126 H H H H Cl CH₃CH₂SCH₂CH₃ H 0 B-2127 H H H H Cl CH₂CH₂CH₂SCH₃ H 0 B-2128 H H H H Cl CH₂CH₂CH₂SCH₂CH₃ H 0 B-2129 H H H H Cl CH(CH₃)SCH₃ H 0 B-2130 H H H H Cl CH(CH₃)SCH₂CH₃ H 0

TABLE 129 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2131 H H H H Cl CH₂CH(CH₃)SCH₃ H 0 B-2132 H H H H Cl CH₂CH(CH₃)SCH₂CH₃ H 0 B-2133 H H H H Cl CH(CH₃)CH₂CH₂SCH₃ H 0 B-2134 H H H H Cl CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-2135 H H H H Cl CH₂CH(CH₃)CH₂SCH₃ H 0 B-2136 H H H H Cl CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-2137 H H H H Cl CH₂CH₂CH(CH₃)SCH₃ H 0 B-2138 H H H H Cl CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-2139 H H H H Cl CH₂SOCH₃ H 0 B-2140 H H H H Cl CH₂CH₂SOCH₃ H 0 B-2141 H H H H Cl CH₂CH₂CH₂SOCH₃ H 0 B-2142 H H H H Cl CH(CH₃)SOCH₃ H 0 B-2143 H H H H Cl CH₂CH(CH₃)SOCH₃ H 0 B-2144 H H H H Cl CH(CH₃)CH₂CH₂SOCH₃ H 0 B-2145 H H H H Cl CH₂CH(CH₃)CH₂SOCH₃ H 0 B-2146 H H H H Cl CH₂CH₂CH(CH₃)SOCH₃ H 0 B-2147 H H H H Cl CH₂SO₂CH₃ H 0 B-2148 H H H H Cl CH₂CH₂SO₂CH₃ H 0 B-2149 H H H H Cl CH₂CH₂CH₂SO₂CH₃ H 0 B-2150 H H H H Cl CH(CH₃)SO₂CH₃ H 0 B-2151 H H H H Cl CH₂CH(CH₃)SO₂CH₃ H 0 B-2152 H H H H Cl CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-2153 H H H H Cl CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-2154 H H H H Cl CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-2155 H H H H Cl CH₂SCF₃ H 0 B-2156 H H H H Cl CH₂SCHF₂ H 0 B-2157 H H H H Cl CH₂SCH₂CF₃ H 0 B-2158 H H H H Cl CH₂SCH₂CHF₂ H 0 B-2159 H H H H Cl CH₂SCF₂CF₃ H 0 B-2160 H H H H Cl CH₂CH₂SCF₃ H 0 B-2161 H H H H Cl CH₂CH₂SCH₂CF₃ H 0 B-2162 H H H H Cl CH₂CH₂CH₂SCF₃ H 0 B-2163 H H H H Cl CH₂CH₂CH₂SCH₂CF₃ H 0 B-2164 H H H H Cl CH(CH₃)SCF₃ H 0 B-2165 H H H H Cl CH(CH₃)SCH₂CF₃ H 0 B-2166 H H H H Cl CH₂CH(CH₃)SCF₃ H 0 B-2167 H H H H Cl CH₂CH(CH₃)SCH₂CF₃ H 0 B-2168 H H H H Cl CH(CH₃)CH₂CH₂SCF₃ H 0 B-2169 H H H H Cl CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-2170 H H H H Cl CH₂CH(CH₃)CH₂SCF₃ H 0 B-2171 H H H H Cl CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-2172 H H H H Cl CH₂CH₂CH(CH₃)SCF₃ H 0 B-2173 H H H H Cl CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-2174 H H H H Cl CH₂SOCF₃ H 0 B-2175 H H H H Cl CH₂CH₂SOCF₃ H 0 B-2176 H H H H Cl CH₂CH₂CH₂SOCF₃ H 0 B-2177 H H H H Cl CH(CH₃)SOCF₃ H 0 B-2178 H H H H Cl CH₂CH(CH₃)SOCF₃ H 0 B-2179 H H H H Cl CH(CH₃)CH₂CH₂SOCF₃ H 0 B-2180 H H H H Cl CH₂CH(CH₃)CH₂SOCF₃ H 0 B-2181 H H H H Cl CH₂CH₂CH(CH₃)SOCF₃ H 0 B-2182 H H H H Cl CH₂SO₂CF₃ H 0 B-2183 H H H H Cl CH₂CH₂SO₂CF₃ H 0 B-2184 H H H H Cl CH₂CH₂CH₂SO₂CF₃ H 0 B-2185 H H H H Cl CH(CH₃)SO₂CF₃ H 0 B-2186 H H H H Cl CH₂CH(CH₃)SO₂CF₃ H 0 B-2187 H H H H Cl CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-2188 H H H H Cl CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-2189 H H H H Cl CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-2190 H H H H Cl CH₂C(═O)CH₃ H 0 B-2191 H H H H Cl CH₂C(═O)CH₂CH₃ H 0

TABLE 130 Compound R¹ r² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2192 H H H H Cl CH₂C(═O)C(CH₃)₃ H 0 B-2193 H H H H Cl CH₂CH₂C(═O)CH₃ H 0 B-2194 H H H H Cl CH₂CH₂C(═O)C(CH₃)₃ H 0 B-2195 H H H H Cl CH₂C(═O)CF₃ H 0 B-2196 H H H H Cl CH₂CH₂C(═O)CF₃ H 0 B-2197 H H H H Cl CH₂C(═O)OCH₃ H 0 B-2198 H H H H Cl CH₂C(═O)OCH₂CH₃ H 0 B-2199 H H H H Cl CH₂C(═O)OC(CH₃)₃ H 0 B-2200 H H H H Cl CH₂CH₂C(═O)OCH₃ H 0 B-2201 H H H H Cl CH₂CH₂C(═O)OCH₂CH₃ H 0 B-2202 H H H H Cl CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-2203 H H H H Cl CH₂C(═O)NH₂ H 0 B-2204 H H H H Cl CH₂CH₂C(═O)NH₂ H 0 B-2205 H H H H Cl CH₂C(═O)NHCH₃ H 0 B-2206 H H H H Cl CH₂C(═O)NHCH(CH₃)₂ H 0 B-2207 H H H H Cl CH₂CH₂C(═O)NHCH₃ H 0 B-2208 H H H H Cl CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-2209 H H H H Cl CH₂C(═O)NHCH₂CHF₂ H 0 B-2210 H H H H Cl CH₂C(═O)NHCH₂CF₃ H 0 B-2211 H H H H Cl CH₂CH₂C(═O)NHCH₂CHF₃ H 0 B-2212 H H H H Cl CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-2213 H H H H Cl CH₂C(═O)N(CH₃)₂ H 0 B-2214 H H H H Cl CH₂C(═O)N(CH₂CH₃)₂ H 0 B-2215 H H H H Cl CH₂CH₂C(═O)N(CH₃)₂ H 0 B-2216 H H H H Cl CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-2217 H H H H Cl CH₂CH₂OH H 0 B-2218 H H H H Cl CH₂CH(OH)CH₃ H 0 B-2219 H H H H Cl CH₂CH₂CH₂OH H 0 B-2220 H H H H Cl CH₂CH(OH)CH₂CH₃ H 0 B-2221 H H H H Cl CH₂CH(OH)C(CH₃)₃ H 0 B-2222 H H H H Cl CH₂CH₂CH(OH)CH₃ H 0 B-2223 H H H H Cl CH₂CH₂CH(OH)C(CH₃)H H 0 B-2224 H H H H Cl CH₂C(═NOH)CH₃ H 0 B-2225 H H H H Cl CH₂C(═NOH)CH₂CH₃ H 0 B-2226 H H H H Cl CH₂C(═NOH)C(CH₃)₃ H 0 B-2227 H H H H Cl CH₂C(═NOCH₃)CH₃ H 0 B-2228 H H H H Cl CH₂C(═NOCH₃)CH₂CH₃ H 0 B-2229 H H H H Cl CH₂C(═NOCH₂CH₃)CH₃ H 0 B-2230 H H H H Cl CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-2231 H H H H Cl CH₂C(═NOCH₂CF₃)CH₃ H 0 B-2232 H H H H Cl CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0 B-2233 H H H H Cl CH₂Ph H 0 B-2234 H H H H Cl CH₂(2-F)Ph H 0 B-2235 H H H H Cl CH₂(3-F)Ph H 0 B-2236 H H H H Cl CH₂(4-F)Ph H 0 B-2237 H H H H Cl CH₂(2-Cl)Ph H 0 B-2238 H H H H Cl CH₂(3-Cl)Ph H 0 B-2239 H H H H Cl CH₂(4-Cl)Ph H 0 B-2240 H H H H Cl CH₂(2-CF₃)Ph H 0 B-2241 H H H H Cl CH₂(3-CF₃)Ph H 0 B-2242 H H H H Cl CH₂(4-CF₃)Ph H 0 B-2243 H H H H Cl CH₂(naphthalen-1-yl) H 0 B-2244 H H H H Cl CH₂(naphthalen-2-yl) H 0 B-2245 H H H H Cl CH₂CH₂Ph H 0 B-2246 H H H H Cl H CH₂CH₃ 0 B-2247 H H H H Cl CH₃ CH₂CH₃ 0 B-2248 H H H H Cl CH₂CH₃ CH₂CH₃ 0 B-2249 H H H H Cl CH(CH₃)₂ CH₂CH₃ 0 B-2250 H H H H Cl CH₂CH₂CH₃ CH₂CH₃ 0 B-2251 H H H H Cl CH₂CH(CH₃)₂ CH₂CH₃ 0 B-2252 H H H H Cl CH₂C(CH₃)₃ CH₂CH₃ 0

TABLE 131 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2253 H H H H Cl CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-2254 H H H H Cl CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-2255 H H H H Cl CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-2256 H H H H Cl CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-2257 H H H H Cl CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-2258 H H H H Cl CH₂OCH₃ CH₂CH₃ 0 B-2259 H H H H Cl CH₂OCH₂CH₃ CH₂CH₃ 0 B-2260 H H H H Cl CH₂CH₂OCH₃ CH₂CH₃ 0 B-2261 H H H H Cl CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-2262 H H H H Cl CF₃ CH₂CH₃ 0 B-2263 H H H H Cl CHF₂ CH₂CH₃ 0 B-2264 H H H H Cl CH₂CF₃ CH₂CH₃ 0 B-2265 H H H H Cl CH₂CHF₂ CH₂CH₃ 0 B-2266 H H H H Cl CH₂CClF₂ CH₂CH₃ 0 B-22S7 H H H H Cl CH₂CBrF₂ CH₂CH₃ 0 B-2268 H H H H Cl CF₂CF₃ CH₂CH₃ 0 B-2269 H H H H Cl CF₂CHF₂ CH₂CH₃ 0 B-2270 H H H H Cl CH₂CH₂CF₃ CH₂CH₃ 0 B-2271 H H H H Cl CH₂CF₂CF₃ CH₂CH₃ 0 B-2272 H H H H Cl CH₂CF₂CHF₂ CH₂CH₃ 0 B-2273 H H H H Cl CF₂CHFCF₃ CH₂CH₃ 0 B-2274 H H H H Cl CF₂CF₂CF₃ CH₂CH₃ 0 B-2275 H H H H Cl CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2276 H H H H Cl CH₂CF₂CHFCF₃ CH₂CH₃ 0 B-2277 H H H H Cl CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2278 H H H H Cl CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-2279 H H H H Cl CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2280 H H H H Cl CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-2281 H H H H Cl CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2282 H H H H Cl CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2283 H H H H Cl CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2284 H H H H Cl CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-2285 H H H H Cl CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-2286 H H H H Cl CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2287 H H H H Cl CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2288 H H H H Cl CF₂CHFOCH₃ CH₂CH₃ 0 B-2289 H H H H Cl CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-2290 H H H H Cl CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-2291 H H H H Cl CF₂CHFOCF₃ CH₂CH₃ 0 B-2292 H H H H Cl CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-2293 H H H H Cl CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-2294 H H H H Cl CH₂CH═CH₂ CH₂CH₃ 0 B-2295 H H H H Cl CH₂CH═CHCl CH₂CH₃ 0 B-2296 H H H H Cl CH₂CH═CCl₂ CH₂CH₃ 0 B-2297 H H H H Cl CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-2298 H H H H Cl CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-2299 H H H H Cl CH₂C≡CH CH₂CH₃ 0 B-2300 H H H H Cl CH₂C≡CCH₃ CH₂CH₃ 0 B-2301 H H H H Cl CH₂C≡Cl CH₂CH₃ 0 B-2302 H H H H Cl CH₂C≡CCF₃ CH₂CH₃ 0 8-2303 H H H H Cl cyclobutyl CH₂CH₃ 0 B-2304 H H H H Cl cyclopentyl CH₂CH₃ 0 B-2305 H H H H Cl cyclohexyl CH₂CH₃ 0 B-2306 H H H H Cl 4,4-difluorocyclohexyl CH₂CH₃ 0 B-2307 H H H H Cl CH₂(cyclopropyl) CH₂CH₃ 0 B-2308 H H H H Cl CH₂(cyclobutyl) CH₂CH₃ 0 B-2309 H H H H Cl CH₂(cyclopentyl) CH₂CH₃ 0 B-2310 H H H H Cl CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-2311 H H H H Cl CH₂(2,2-difluorocydopropyl) CH₂CH₃ 0 B-2312 H H H H Cl CH₂(2,2-dichlorocydopropyl) CH₂CH₃ 0 B-2313 H H H H Cl CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0

TABLE 132 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2314 H H H H Cl CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-2315 H H H H Cl CH₂CH₂(2,2-dichlorocyclopropyl) CH₃CH₃ 0 B-2316 H H H H Cl CH₂SCH₃ CH₂CH₃ 0 B-2317 H H H H Cl CH₂SCH₂CH₃ CH₂CH₃ 0 B-2318 H H H H Cl CH₂CH₂SCH₃ CH₂CH₃ 0 B-2319 H H H H Cl CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-2320 H H H H Cl CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-2321 H H H H Cl CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-2322 H H H H Cl CH(CH₃)SCH₃ CH₂CH₃ 0 B-2323 H H H H Cl CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-2324 H H H H Cl CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-2325 H H H H Cl CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-2326 H H H H Cl CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-2327 H H H H Cl CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-2328 H H H H Cl CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-2329 H H H H Cl CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-2330 H H H H Cl CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-2331 H H H H Cl CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-2332 H H H H Cl CH₂SOCH₃ CH₂CH₃ 0 B-2333 H H H H Cl CH₂CH₂SOCH₃ CH₂CH₃ 0 B-2334 H H H H Cl CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-2335 H H H H Cl CH(CH₃)SOCH₃ CH₂CH₃ 0 B-2336 H H H H Cl CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-2337 H H H H Cl CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-2338 H H H H Cl CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-2339 H H H H Cl CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-2340 H H H H Cl CH₂SO₂CH₃ CH₂CH₃ 0 B-2341 H H H H Cl CH₂H₂SO₂CH₃ CH₂CH₃ 0 B-2342 H H H H Cl CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-2343 H H H H Cl CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-2344 H H H H Cl CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-2345 H H H H Cl CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-2346 H H H H Cl CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-2347 H H H H Cl CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-2348 H H H H Cl CH₂SCF₃ CH₂CH₃ 0 B-2349 H H H H Cl CH₂SCHF₂ CH₂CH₃ 0 B-2350 H H H H Cl CH₂SCH₂CF₃ CH₂CH₃ 0 B-2351 H H H H Cl CH₂SCH₂CHF₂ CH₂CH₃ 0 B-2352 H H H H Cl CH₂SCF₂CF₃ CH₂CH₃ 0 B-2353 H H H H Cl CH₂CH₂SCF₃ CH₂CH₃ 0 B-2354 H H H H Cl CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-2355 H H H H Cl CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-2356 H H H H Cl CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-2357 H H H H Cl CH(CH₃)SCF₃ CH₂CH₃ 0 B-2358 H H H H Cl CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-2359 H H H H Cl CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-2360 H H H H Cl CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-2361 H H H H Cl CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-2362 H H H H Cl CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-2363 H H H H Cl CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-2364 H H H H Cl CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-2365 H H H H Cl CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-2366 H H H H Cl CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-2367 H H H H Cl CH₂SOCF₃ CH₂CH₃ 0 B-2368 H H H H Cl CH₂CH₂SOCF₃ CH₂CH₃ 0 B-2369 H H H H Cl CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-2370 H H H H Cl CH(CH₃)SOCF₃ CH₂CH₃ 0 B-2371 H H H H Cl CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-2372 H H H H Cl CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-2373 H H H H Cl CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-2374 H H H H Cl CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0

TABLE 133 Compound R¹ R³ R³ R⁴ R⁵ R⁶ R¹⁶ n B-2375 H H H H Cl CH₂SO₂CF₃ CH₂CH₃ 0 B-2376 H H H H Cl CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-2377 H H H H Cl CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-2378 H H H H Cl CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-2379 H H H H Cl CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-2380 H H H H Cl CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-2381 H H H H Cl CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-2382 H H H H Cl CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-2383 H H H H Cl CH₂C(═O)CH₃ CH₂CH₃ 0 B-2384 H H H H Cl CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-2385 H H H H Cl CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-2386 H H H H Cl CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-2387 H H H H Cl CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-2388 H H H H Cl CH₂C(═O)CF₃ CH₂CH₃ 0 B-2389 H H H H Cl CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-2390 H H H H Cl CH₂C(═O)OCH₃ CH₂CH₃ 0 B-2391 H H H H Cl CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-2392 H H H H Cl CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-2393 H H H H Cl CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-2394 H H H H Cl CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-2395 H H H H Cl CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-2396 H H H H Cl CH₂C(═O)NH₂ CH₂CH₃ 0 B-2397 H H H H Cl CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-2398 H H H H Cl CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-2399 H H H H Cl CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-2400 H H H H Cl CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-2401 H H H H Cl CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-2402 H H H H Cl CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-2403 H H H H Cl CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-2404 H H H H Cl CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-2405 H H H H Cl CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-2406 H H H H Cl CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-2407 H H H H Cl CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-2408 H H H H Cl CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-2409 H H H H Cl CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-2410 H H H H Cl CH₂CH₂OH CH₂CH₃ 0 B-2411 H H H H Cl CH₂CH(OH)CH₃ CH₂CH₃ 0 B-2412 H H H H Cl CH₂CH₂CH₂OH CH₂CH₃ 0 B-2413 H H H H Cl CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-2414 H H H H Cl CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-2415 H H H H Cl CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0 B-2416 H H H H Cl CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-2417 H H H H Cl CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-2418 H H H H Cl CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-2419 H H H H Cl CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-2420 H H H H Cl CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-2421 H H H H Cl CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-2422 H H H H Cl CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-2423 H H H H Cl CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-2424 H H H H Cl CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-2425 H H H H Cl CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-2426 H H H H Cl CH₂Ph CH₂CH₃ 0 B-2427 H H H H Cl CH₂(2-F)Ph CH₂CH₃ 0 B-2428 H H H H Cl CH₂(3-F)Ph CH₂CH₃ 0 B-2429 H H H H Cl CH₂(4-F)Ph CH₂CH₃ 0 B-2430 H H H H Cl CH₂(2-Cl)Ph CH₂CH₃ 0 B-2431 H H H H Cl CH₂(3-Cl)Ph CH₂CH₃ 0 B-2432 H H H H Cl CH₂(4-Cl)Ph CH₂CH₃ 0 B-2433 H H H H Cl CH₂(2-CF₃)Ph CH₂CH₃ 0 B-2434 H H H H Cl CH₂(3-CF₃)Ph CH₂CH₃ 0 B-2435 H H H H Cl CH₂(4-CF₃)Ph CH₂CH₃ 0

TABLE 134 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2436 H H H H Cl CH₂(naphthalen-1-yl) CH₂CH₃ 0 B-2437 H H H H Cl CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-2438 H H H H Cl CH₂CH₂Ph CH₂CH₃ 0 B-2439 H H H H F H H 0 B-2440 H H H H F CH₃ H 0 B-2441 H H H H F CH₂CH₃ H 0 B-2442 H H H H F CH(CH₃)₂ H 0 B-2443 H H H H F CH₂CH₂CH₃ H 0 B-2444 H H H H F CH₂CH(CH₃)₂ H 0 B-2445 H H H H F CH₂C(CH₃)₃ H 0 B-2446 H H H H F CH(CH₃)CH₂CH₃ H 0 B-2447 H H H H F CH₂(CH₂)₂CH₃ H 0 B-2448 H H H H F CH₂(CH₂)₃CH₃ H 0 B-2449 H H H H F CH₂(CH₂)₄CH₃ H 0 B-2450 H H H H F CH₂(CH₂)₆CH₃ H 0 B-2451 H H H H F CH₂OCH₃ H 0 B-2452 H H H H F CH₂OCH₂CH₃ H 0 B-2453 H H H H F CH₂CH₂OCH₃ H 0 B-2454 H H H H F CH₂CH₂OCH₂CH₃ H 0 B-2455 H H H H F CF₃ H 0 B-2456 H H H H F CHF₂ H 0 B-2457 H H H H F CH₂CF₃ H 0 B-2458 H H H H F CH₂CHF₂ H 0 B-2459 H H H H F CH₃CClF₂ H 0 B-2460 H H H H F CH₂CBrF₂ H 0 B-2461 H H H H F CF₂CF₃ H 0 B-2462 H H H H F CF₂CHF₂ H 0 B-2463 H H H H F CH₂CH₃CF₃ H 0 B-2464 H H H H F CH₂CF₂CF₃ H 0 B-2465 H H H H F CH₂CF₂CHF₂ H 0 B-2466 H H H H F CF₂CHFCF₃ H 0 B-2467 H H H H F CF₂CF₂CF₃ H 0 B-2468 H H H H F CH₂CF₂CF₂CF₃ H 0 B-2469 H H H H F CH₂CF₂CHFCF₃ H 0 B-2470 H H H H F CH₂CH₂CH₂CF₃ H 0 B-2471 H H H H F CH₂CH₂CF₂CF₃ H 0 B-2472 H H H H F CF₂CF₂CF₂CF₃ H 0 B-2473 H H H H F CH₂CH₂CH(CF₃)₂ H 0 B-2474 H H H H F CF₂CF₂CF₂CF₂CF₃ H 0 B-2475 H H H H F CH₂CF₂CF₂CF₂CF₃ H 0 B-2476 H H H H F CH₂CH₂CH₂CH₂CF₃ H 0 B-2477 H H H H F CH₂CF₂CF₂CF₂CHF₂ H 0 B-2478 H H H H F CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-2479 H H H H F CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-2480 H H H H F CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-2481 H H H H F CF₂CHFOCH₃ H 0 B-2482 H H H H F CF₂CHFOCH₂CH₃ H 0 B-2483 H H H H F CH₂CH₂OCH₂CF₃ H 0 B-2484 H H H H F CF₂CHFOCF₃ H 0 B-2485 H H H H F CF₂CHFOCF₂CF₃ H 0 B-2486 H H H H F CF₂CHFOCF₂CF₂CF₃ H 0 B-2487 H H H H F CH₂CH═CH₂ H 0 B-2488 H H H H F CH₂CH═CHCl H 0 B-2489 H H H H F CH₂CH═CCl₂ H 0 B-2490 H H H H F CH₂CH₂CF═CF₂ H 0 B-2491 H H H H F CH₂CH₂CH═CF₂ H 0 B-2492 H H H H F CH₂C≡CH H 0 B-2493 H H H H F CH₂C≡CCH₃ H 0 B-2494 H H H H F CH₂C≡Cl H 0 B-2495 H H H H F CH₂C≡CCF₃ H 0 B-2496 H H H H F cyclobutyl H 0

TABLE 135 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2497 H H H H F cyclopentyl H 0 B-2498 H H H H F cyclohexyl H 0 B-2499 H H H H F 4,4-difluorocyclohexyl H 0 B-2500 H H H H F CH₂(cyclopropyl) H 0 B-2501 H H H H F CH₂(cyclobutyl) H 0 B-2502 H H H H F CH₂(cyclopentyl) H 0 B-2503 H H H H F CH₂CH₂(cyclopropyl) H 0 B-2504 H H H H F CH₂(2,2-difluorocyclopropyl) H 0 B-2505 H H H H F CH₂(2,2-dichlorocydopropyl) H 0 B-2506 H H H H F CH₂(4,4-difluorocyclohexyl) H 0 B-2507 H H H H F CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-2508 H H H H F CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-2509 H H H H F CH₂SCH₃ H 0 B-2510 H H H H F CH₂SCH₂CH₃ H 0 B-2511 H H H H F CH₂CH₂SCH₃ H 0 B-2512 H H H H F CH₂CH₂SCH₂CH₃ H 0 B-2513 H H H H F CH₂CH₂CH₂SCH₃ H 0 B-2514 H H H H F CH₂CH₂CH₂SCH₂CH₃ H 0 B-2515 H H H H F CH(CH₃)SCH₃ H 0 B-2516 H H H H F CH(CH₃)SCH₂CH₃ H 0 B-2517 H H H H F CH₂CH(CH₃)SCH₃ H 0 B-2518 H H H H F CH₂CH(CH₃)SCH₂CH₃ H 0 B-2519 H H H H F CH(CH₃)CH₂CH₂SCH₃ H 0 B-2520 H H H H F CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-2521 H H H H F CH₂CH(CH₃)CH₂SCH₃ H 0 B-2522 H H H H F CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-2523 H H H H F CH₂CH₂CH(CH₃)SCH₃ H 0 B-2524 H H H H F CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-2525 H H H H F CH₂SOCH₃ H 0 B-2526 H H H H F CH₂CH₂SOCH₃ H 0 B-2527 H H H H F CH₂CH₂CH₂SOCH₃ H 0 B-2528 H H H H F CH(CH₃)SOCH₃ H 0 B-2529 H H H H F CH₂CH(CH₃)SOCH₃ H 0 B-2530 H H H H F CH(CH₃)CH₂CH₂SOCH₃ H 0 B-2531 H H H H F CH₂CH(CH₃)CH₂SOCH₃ H 0 B-2532 H H H H F CH₂CH₂CH(CH₃)SOCH₃ H 0 B-2533 H H H H F CH₂SO₂CH₃ H 0 B-2534 H H H H F CH₂CH₂SO₂CH₃ H 0 B-2535 H H H H F CH₂CH₂CH₂SO₂CH₃ H 0 B-2536 H H H H F CH(CH₃)SO₂CH₃ H 0 B-2537 H H H H F CH₂CH(CH₃)SO₂CH₃ H 0 B-2538 H H H H F CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-2539 H H H H F CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-2540 H H H H F CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-2541 H H H H F CH₂SCF₃ H 0 B-2542 H H H H F CH₂SCHF₂ H 0 B-2543 H H H H F CH₂SCH₂CF₃ H 0 B-2544 H H H H F CH₂SCH₂CHF₂ H 0 B-2545 H H H H F CH₂SCF₂CF₃ H 0 B-2546 H H H H F CH₂CH₂SCF₃ H 0 B-2547 H H H H F CH₂CH₂SCH₂CF₃ H 0 B-2548 H H H H F CH₂CH₂CH₂SCF₃ H 0 B-2549 H H H H F CH₂CH₂CH₂SCH₂CF₃ H 0 B-2550 H H H H F CH(CH₃)SCF₃ H 0 B-2551 H H H H F CH(CH₃)SCH₂CF₃ H 0 B-2552 H H H H F CH₂CH(CH₃)SCF₃ H 0 B-2553 H H H H F CH₂CH(CH₃)SCH₂CF₃ H 0 B-2554 H H H H F CH(CH₃)CH₂CH₂SCF₃ H 0 B-2555 H H H H F CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-2556 H H H H F CH₂CH(CH₃)CH₂SCF₃ H 0 B-2557 H H H H F CH₂CH(CH₃)CH₂SCH₂CF₃ H 0

TABLE 136 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2558 H H H H F CH₂CH₂CH(CH₃)SCF₃ H 0 B-2559 H H H H F CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-2560 H H H H F CH₂SOCF₃ H 0 B-2561 H H H H F CH₂CH₂SOCF₃ H 0 B-2562 H H H H F CH₂CH₂CH₂SOCF₃ H 0 B-2563 H H H H F CH(CH₃)SOCF₃ H 0 B-2564 H H H H F CH₂CH(CH₃)SOCF₃ H 0 B-2565 H H H H F CH(CH₃)CH₂CH₂SOCF₃ H 0 B-2566 H H H H F CH₂CH(CH₃)CH₂SOCF₃ H 0 B-2567 H H H H F CH₂CH₂CH(CH₃)SOCF₃ H 0 B-2568 H H H H F CH₂SO₂CF₃ H 0 B-2569 H H H H F CH₂CH₂SO₂CF₃ H 0 B-2570 H H H H F CH₂CH₂CH₂SO₂CF₃ H 0 B-2571 H H H H F CH(CH₃)SO₂CF₃ H 0 B-2572 H H H H F CH₂CH(CH₃)SO₂CF₃ H 0 B-2573 H H H H F CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-2574 H H H H F CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-2575 H H H H F CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-2576 H H H H F CH₂C(═O)CH₃ H 0 B-2577 H H H H F CH₂C(═O)CH₂CH₃ H 0 B-2578 H H H H F CH₂C(═O)C(CH₃)₃ H 0 B-2579 H H H H F CH₂CH₂C(═O)CH₃ H 0 B-2580 H H H H F CH₂CH₂C(═O)C(CH₃)₃ H 0 B-2581 H H H H F CH₂C(═O)CF₃ H 0 B-2582 H H H H F CH₂CH₂C(═O)CF₃ H 0 B-2583 H H H H F CH₂C(═O)OCH₃ H 0 B-2584 H H H H F CH₂C(═O)OCH₂CH₃ H 0 B-2585 H H H H F CH₂C(═O)OC(CH₃)₃ H 0 B-2586 H H H H F CH₂CH₂C(═O)OCH₃ H 0 B-2587 H H H H F CH₂CH₂C(═O)OCH₂CH₃ H 0 B-2588 H H H H F CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-2589 H H H H F CH₂C(═O)NH₂ H 0 B-2590 H H H H F CH₂CH₂C(═O)NH₂ H 0 B-2591 H H H H F CH₂C(═O)NHCH₃ H 0 B-2592 H H H H F CH₂C(═O)NHCH(CH₃)₂ H 0 B-2593 H H H H F CH₂CH₂C(═O)NHCH₃ H 0 B-2594 H H H H F CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-2595 H H H H F CH₂C(═O)NHCH₂CHF₂ H 0 B-2596 H H H H F CH₂C(═O)NHCH₂CF₃ H 0 B-2597 H H H H F CH₂CH₂C(═O)NHCH₂CHF₂ H 0 B-2598 H H H H F CH₂CH₂C(═O)NHCH₂CF₃ H 0 B-2599 H H H H F CH₂C(═O)N(CH₃)₂ H 0 B-2600 H H H H F CH₂C(═O)N(CH₂CH₃)₂ H 0 B-2601 H H H H F CH₂CH₂C(═O)N(CH₃)₂ H 0 B-2602 H H H H F CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-2603 H H H H F CH₂CH₂OH H 0 B-2604 H H H H F CH₂CH(OH)CH₃ H 0 B-2605 H H H H F CH₂CH₂CH₂OH H 0 B-2606 H H H H F CH₂CH(OH)CH₂CH₃ H 0 B-2607 H H H H F CH₂CH(OH)C(CH₃)₃ H 0 B-2608 H H H H F CH₂CH₂CH(OH)CH₃ H 0 B-2609 H H H H F CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-2610 H H H H F CH₂C(═NOH)CH₃ H 0 B-2611 H H H H F CH₂C(═NOH)CH₂CH₃ H 0 B-2612 H H H H F CH₂C(═NOH)C(CH₃)₃ H 0 B-2613 H H H H F CH₂C(═NOCH₃)CH₃ H 0 B-2614 H H H H F CH₂C(═NOCH₃)CH₂CH₃ H 0 B-2615 H H H H F CH₂C(═NOCH₂CH₃)CH₃ H 0 B-2616 H H H H F CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-2617 H H H H F CH₂C(═NOCH₂CF₃)CH₃ H 0 B-2618 H H H H F CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0

TABLE 137 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2619 H H H H F CH₂Ph H 0 B-2620 H H H H F CH₂(2-F)Ph H 0 B-2621 H H H H F CH₂(3-F)Ph H 0 B-2622 H H H H F CH₂(4-F)Ph H 0 B-2623 H H H H F CH₂(2-Cl)Ph H 0 B-2624 H H H H F CH₂(3-Cl)Ph H 0 B-2625 H H H H F CH₂(4-Cl)Ph H 0 B-2626 H H H H F CH₂(2-CF₃)Ph H 0 B-2627 H H H H F CH₂(3-CF₃)Ph H 0 B-2628 H H H H F CH₂(4-CF₃)Ph H 0 B-2629 H H H H F CH₂(naphthalen-1-yl) H 0 B-2630 H H H H F CH₂(naphthalen-2-yl) H 0 B-2631 H H H H F CH₂CH₂Ph H 0 B-2632 H H H H F H CH₂CH₃ 0 B-2633 H H H H F CH₃ CH₂CH₃ 0 B-2634 H H H H F CH₂CH₃ CH₂CH₃ 0 B-2635 H H H H F CH(CH₃)₂ CH₂CH₃ 0 B-2636 H H H H F CH₂CH₂CH₃ CH₂CH₃ 0 B-2637 H H H H F CH₂CH(CH₃)₂ CH₂CH₃ 0 B-2638 H H H H F CH₂C(CH₃)₃ CH₂CH₃ 0 B-2639 H H H H F CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-2640 H H H H F CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-2641 H H H H F CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-2642 H H H H F CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-2643 H H H H F CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-2644 H H H H F CH₂OCH₃ CH₂CH₃ 0 B-2645 H H H H F CH₂OCH₂CH₃ CH₂CH₃ 0 B-2646 H H H H F CH₂CH₂OCH₃ CH₂CH₃ 0 B-2647 H H H H F CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-2648 H H H H F CF₃ CH₂CH₃ 0 B-2649 H H H H F CHF₂ CH₂CH₃ 0 B-2650 H H H H F CH₂CF₃ CH₂CH₃ 0 B-2651 H H H H F CH₂CHF₂ CH₂CH₃ 0 B-2652 H H H H F CH₂CClF₂ CH₂CH₃ 0 B-2653 H H H H F CH₂CBrF₂ CH₂CH₃ 0 B-2654 H H H H F CF₂CF₃ CH₂CH₃ 0 B-2655 H H H H F CF₂CHF₂ CH₂CH₃ 0 B-2656 H H H H F CH₂CH₂CF₃ CH₂CH₃ 0 B-2657 H H H H F CH₂CF₂CF₃ CH₂CH₃ 0 B-2658 H H H H F CH₂CF₂CHF₂ CH₂CH₃ 0 B-2659 H H H H F CF₂CHFCF₃ CH₂CH₃ 0 B-2660 H H H H F CF₂CF₂CF₃ CH₂CH₃ 0 B-2661 H H H H F CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2662 H H H H F CH₂CF₂CHFCF₃ CH₂CH₃ 0 B-2663 H H H H F CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2664 H H H H F CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-2665 H H H H F CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2666 H H H H F CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-2667 H H H H F CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2668 H H H H F CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-2669 H H H H F CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2670 H H H H F CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-2671 H H H H F CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-2672 H H H H F CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2673 H H H H F CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-2674 H H H H F CF₂CHFOCH₃ CH₂CH₃ 0 B-2675 H H H H F CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-2676 H H H H F CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-2677 H H H H F CF₂CHFOCF₃ CH₂CH₃ 0 B-2678 H H H H F CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-2679 H H H H F CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0

TABLE 138 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2680 H H H H F CH₂CH═CH₂ CH₂CH₃ 0 B-2681 H H H H F CH₂CH═CHCl CH₂CH₃ 0 B-2682 H H H H F CH₂CH═CCl₂ CH₂CH₃ 0 B-2683 H H H H F CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-2684 H H H H F CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-2685 H H H H F CH₂C≡CH CH₂CH₃ 0 B-2686 H H H H F CH₂C≡CCH₃ CH₂CH₃ 0 B-2687 H H H H F CH₂C≡Cl CH₂CH₃ 0 B-2688 H H H H F CH₂C≡CCF₃ CH₂CH₃ 0 B-2689 H H H H F cyclobutyl CH₂CH₃ 0 B-2690 H H H H F cyclcpentyl CH₂CH₃ 0 B-2691 H H H H F cyclohexyl CH₂CH₃ 0 B-2692 H H H H F 4,4-difluorocyclohexyl CH₂CH₃ 0 B-2693 H H H H F CH₂(cyclopropyl) CH₂CH₃ 0 B-2694 H H H H F CH₂(cyclobutyl) CH₂CH₃ 0 B-2695 H H H H F CH₂(cyclopentyl) CH₂CH₃ 0 B-2696 H H H H F CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-2697 H H H H F CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-2698 H H H H F CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-2699 H H H H F CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-2700 H H H H F CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-2701 H H H H F CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-2702 H H H H F CH₂SCH₃ CH₂CH₃ 0 B-2703 H H H H F CH₂SCH₂CH₃ CH₂CH₃ 0 B-2704 H H H H F CH₂CH₂SCH₃ CH₂CH₃ 0 B-2705 H H H H F CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-2706 H H H H F CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-2707 H H H H F CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-2708 H H H H F CH(CH₃)SCH₃ CH₂CH₃ 0 B-2709 H H H H F CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-2710 H H H H F CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-2711 H H H H F CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-2712 H H H H F CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-2713 H H H H F CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-2714 H H H H F CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-2715 H H H H F CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-2716 H H H H F CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-2717 H H H H F CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-2718 H H H H F CH₂SOCH₃ CH₂CH₃ 0 B-2719 H H H H F CH₂CH₂SOCH₃ CH₂CH₃ 0 B-2720 H H H H F CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0 B-2721 H H H H F CH(CH₃)SOCH₃ CH₂CH₃ 0 B-2722 H H H H F CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-2723 H H H H F CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-2724 H H H H F CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-2725 H H H H F CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-2726 H H H H F CH₂SO₂CH₃ CH₂CH₃ 0 B-2727 H H H H F CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-2728 H H H H F CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-2729 H H H H F CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-2730 H H H H F CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-2731 H H H H F CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-2732 H H H H F CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-2733 H H H H F CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-2734 H H H H F CH₂SCF₃ CH₂CH₃ 0 B-2735 H H H H F CH₂SCHF₂ CH₂CH₃ 0 B-2736 H H H H F CH₂SCH₂CF₃ CH₂CH₃ 0 B-2737 H H H H F CH₂SCH₂CHF₂ CH₂CH₃ 0 B-2738 H H H H F CH₂SCF₂CF₃ CH₂CH₃ 0 B-2739 H H H H F CH₂CH₂SCF₃ CH₂CH₃ 0 B-2740 H H H H F CH₂CH₂SCH₂CF₃ CH₂CH₃ 0

TABLE 139 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2741 H H H H F CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-2742 H H H H F CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-2743 H H H H F CH(CH₃)SCF₃ CH₂CH₃ 0 B-2744 H H H H F CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-2745 H H H H F CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-2746 H H H H F CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-2747 H H H H F CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-2748 H H H H F CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-2749 H H H H F CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-2750 H H H H F CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-2751 H H H H F CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-2752 H H H H F CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-2753 H H H H F CH₂SOCF₃ CH₂CH₃ 0 B-2754 H H H H F CH₂CH₂SOCF₃ CH₂CH₃ 0 B-2755 H H H H F CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-2756 H H H H F CH(CH₃)SOCF₃ CH₂CH₃ 0 B-2757 H H H H F CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-2758 H H H H F CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-2759 H H H H F CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-2760 H H H H F CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-2761 H H H H F CH₂SO₂CF₃ CH₂CH₃ 0 B-2762 H H H H F CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-2763 H H H H F CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-2764 H H H H F CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-2765 H H H H F CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-2765 H H H H F CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-2767 H H H H F CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-2768 H H H H F CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-2769 H H H H F CH₂C(═O)CH₃ CH₂CH₃ 0 B-2770 H H H H F CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-2771 H H H H F CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-2772 H H H H F CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-2773 H H H H F CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-2774 H H H H F CH₂C(═O)CF₃ CH₂CH₃ 0 B-2775 H H H H F CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-2776 H H H H F CH₂C(═O)OCH₃ CH₂CH₃ 0 B-2777 H H H H F CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-2778 H H H H F CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-2779 H H H H F CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-2780 H H H H F CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-2781 H H H H F CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-2782 H H H H F CH₂C(═O)NH₂ CH₂CH₃ 0 B-2783 H H H H F CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-2784 H H H H F CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-2785 H H H H F CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-2786 H H H H F CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-2787 H H H H F CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-2788 H H H H F CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-2789 H H H H F CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-2790 H H H H F CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-2791 H H H H F CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-2792 H H H H F CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-2793 H H H H F CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-2794 H H H H F CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-2795 H H H H F CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-2796 H H H H F CH₂CH₂OH CH₂CH₃ 0 B-2797 H H H H F CH₂CH(OH)CH₃ CH₂CH₃ 0 B-2798 H H H H F CH₂CH₂CH₂OH CH₂CH₃ 0 B-2799 H H H H F CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-2800 H H H H F CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-2801 H H H H F CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0

TABLE 140 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2802 H H H H F CH₂CH₃CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-2803 H H H H F CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-2804 H H H H F CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-2805 H H H H F CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-2806 H H H H F CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-2807 H H H H F CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-2808 H H H H F CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-2809 H H H H F CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-2810 H H H H F CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-2811 H H H H F CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-2812 H H H H F CH₂Ph CH₂CH₃ 0 B-2813 H H H H F CH₂(2-F)Ph CH₂CH₃ 0 B-2814 H H H H F CH₂(3-F)Ph CH₂CH₃ 0 B-2815 H H H H F CH₂(4-F)Ph CH₂CH₃ 0 B-2816 H H H H F CH₂(2-Cl)Ph CH₂CH₃ 0 B-2817 H H H H F CH₂(3-Cl)Ph CH₂CH₃ 0 B-2818 H H H H F CH₂(4-Cl)Ph CH₂CH₃ 0 B-2819 H H H H F CH₂(2-CF₃)Ph CH₂CH₃ 0 B-2820 H H H H F CH₂(3-CF₃)Ph CH₂CH₃ 0 B-2821 H H H H F CH₂(4-CF₃)Ph CK₂CH₃ 0 B-2822 H H H H F CH₂(naphthalen-1-yl) CH₂CH₃ 0 B-2823 H H H H F CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-2824 H H H H F CH₂CH₂Ph CH₂CH₃ 0 B-2825 H H H H CH₃ H H 0 B-2826 H H H H CH₃ CH₃ H 0 B-2827 H H H H CH₃ CH₂CH₃ H 0 B-2828 H H H H CH₃ CH(CH₃)₂ H 0 B-2829 H H H H CH₃ CH₂CH₂CH₃ H 0 B-2830 H H H H CH₃ CH₂CH(CH₃)₂ H 0 B-2831 H H H H CH₃ CH₂C(CH₃)₃ H 0 B-2832 H H H H CH₃ CH(CH₃)CH₂CH₃ H 0 B-2833 H H H H CH₃ CH₂(CH₂)₂CH₃ H 0 B-2834 H H H H CH₃ CH₂(CH₂)₃CH₃ H 0 B-2835 H H H H CH₃ CH₂(CH₂)₄CH₃ H 0 B-2836 H H H H CH₃ CH(CH₂)₆CH₃ H 0 B-2837 H H H H CH₃ CH₂OCH₃ H 0 B-2838 H H H H CH₃ CH₂OCH₂CH₃ H 0 B-2839 H H H H CH₃ CH₂CH₂OCH₃ H 0 B-2840 H H H H CH₃ CH₂CH₂OCH₂CH₃ H 0 B-2841 H H H H CH₃ CF₃ H 0 B-2842 H H H H CH₃ CHF₂ H 0 B-2843 H H H H CH₃ CH₂CF₃ H 0 B-2844 H H H H CH₃ CH₂CHF₂ H 0 B-2845 H H H H CH₃ CH₂CClF₂ H 0 B-2846 H H H H CH₃ CH₂CBrF₂ H 0 B-2847 H H H H CH₃ CF₂CF₃ H 0 B-2848 H H H H CH₃ CF₂CHF₂ H 0 B-2849 H H H H CH₃ CH₂CH₂CF₃ H 0 B-2850 H H H H CH₃ CH₂CF₂CF₃ H 0 B-2851 H H H H CH₃ CH₂CF₂CHF₂ H 0 B-2852 H H H H CH₃ CF₂CHFCF₃ H 0 B-2853 H H H H CH₃ CF₂CF₂CF₃ H 0 B-2854 H H H H CH₃ CH₂CF₂CF₂CF₃ H 0 B-2855 H H H H CH₃ CH₂CF₂CHFCF₃ H 0 B-2856 H H H H CH₃ CH₂CH₂CH₂CF₃ H 0 B-2857 H H H H CH₃ CH₂CH₂CF₂CF₃ H 0 B-2858 H H H H CH₃ CF₂CF₂CF₂CF₃ H 0 B-2859 H H H H CH₃ CH₂CH₂CH(CF₃)₂ H 0 B-2860 H H H H CH₃ CF₂CF₂CF₂CF₂CF₃ H 0 B-2861 H H H H CH₃ CH₂CF₂CF₂CF₂CF₃ H 0 B-2862 H H H H CH₃ CH₂CH₂CH₂CH₂CF₃ H 0

TABLE 141 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2863 H H H H CH₃ CH₂CF₂CF₂CF₂CHF₂ H 0 B-2864 H H H H CH₃ CH₃CF₂CF(CF₃)CF₂C(CF₃)₃ H 0 B-2865 H H H H CH₃ CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-2866 H H H H CH₃ CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 0 B-2867 H H H H CH₃ CF₂CHFOCH₃ H 0 B-2868 H H H H CH₃ CF₂CHFOCH₂CH₃ H 0 B-2869 H H H H CH₃ CH₂CH₂OCH₂CF₃ H 0 B-2870 H H H H CH₃ CF₂CHFOCF₃ H 0 B-2871 H H H H CH₃ CF₂CHFOCF₂CF₃ H 0 B-2872 H H H H CH₃ CF₂CHFOCF₂CF₂CF₃ H 0 B-2873 H H H H CH₃ CH₂CH═CH₂ H 0 B-2874 H H H H CH₃ CH₂CH═CHCl H 0 B-2875 H H H H CH₃ CH₂CH═CCl₂ H 0 B-2876 H H H H CH₃ CH₂CH₂CF═CF₂ H 0 B-2877 H H H H CH₃ CH₂CH₂CH═CF₂ H 0 B-2878 H H H H CH₃ CH₂C≡CH H 0 B-2879 H H H H CH₃ CH₂C≡CCH₃ H 0 B-2880 H H H H CH₃ CH₂C≡Cl H 0 B-2881 H H H H CH₃ CH₂C≡CCF₃ H 0 B-2882 H H H H CH₃ cyclobutyl H 0 B-2883 H H H H CH₃ cyclopentyl H 0 B-2884 H H H H CH₃ cyclohexyl H 0 B-2885 H H H H CH₃ 4,4-difluorocyclohexyl H 0 B-2886 H H H H CH₃ CH₂(cyclopropyl) H 0 B-2887 H H H H CH₃ CH₂(cyclobutyl) H 0 B-2888 H H H H CH₃ CH₂(cydopentyl) H 0 B-2889 H H H H CH₃ CH₂CH₂(cyclopropyl) H 0 B-2890 H H H H CH₃ CH₂(2,2-difluorocyclopropyl) H 0 B-2891 H H H H CH₃ CH₂(2,2-dichlorocyclopropyl) H 0 B-2892 H H H H CH₃ CH₂(4,4-difluorocyclohexyl) H 0 B-2893 H H H H CH₃ CH₂CH₂(2,2-difluorocyclopropyl) H 0 B-2894 H H H H CH₃ CH₂CH₂(2,2-dichlorocyclopropyl) H 0 B-2895 H H H H CH₃ CH₂SCH₃ H 0 B-2896 H H H H CH₃ CH₂SCH₂CH₃ H 0 B-2897 H HI H H CH₃ CH₂CH₂SCH₃ H 0 B-2898 H H H H CH₃ CH₂CH₂SCH₂CH₃ H 0 B-2899 H H H H CH₃ CH₂CH₂CH₂SCH₃ H 0 B-2900 H H H H CH₃ CH₂CH₂CH₂SCH₂CH₃ H 0 B-2901 H H H H CH₃ CH(CH₃)SCH₃ H 0 B-2902 H H H H CH₃ CH(CH₃)SCH₂CH₃ H 0 B-2903 H H H H CH₃ CH₂CH(CH₃)SCH₃ H 0 B-2904 H H H H CH₃ CH₂CH(CH₃)SCH₂CH₃ H 0 B-2905 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₃ H 0 B-2906 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₂CH₃ H 0 B-2907 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₃ H 0 B-2908 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₂CH₃ H 0 B-2909 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₃ H 0 B-2910 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₂CH₃ H 0 B-2911 H H H H CH₃ CH₂SOCH₃ H 0 B-2912 H H H H CH₃ CH₂CH₂SOCH₃ H 0 B-2913 H H H H CH₃ CH₂CH₂CH₂SOCH₃ H 0 B-2914 H H H H CH₃ CH(CH₃)SOCH₃ H 0 B-2915 H H H H CH₃ CH₂CH(CH₃)SOCH₃ H 0 B-2916 H H H H CH₃ CH(CH₃)CH₂CH₂SOCH₃ H 0 B-2917 H H H H CH₃ CH₂CH(CH₃)CH₂SOCH₃ H 0 B-2918 H H H H CH₃ CH₂CH₂CH(CH₃)SOCH₃ H 0 B-2919 H H H H CH₃ CH₂SO₂CH₃ H 0 B-2920 H H H H CH₃ CH₂CH₂SO₂CH₃ H 0 B-2921 H H H H CH₃ CH₂CH₂CH₂SO₂CH₃ H 0 B-2922 H H H H CH₃ CH(CH₃)SO₂CH₃ H 0 B-2923 H H H H CH₃ CH₂CH(CH₃)SO₂CH₃ H 0

TABLE 142 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2924 H H H H CH₃ CH(CH₃)CH₂CH₂SO₂CH₃ H 0 B-2925 H H H H CH₃ CH₂CH(CH₃)CH₂SO₂CH₃ H 0 B-2926 H H H H CH₃ CH₂CH₂CH(CH₃)SO₂CH₃ H 0 B-2927 H H H H CH₃ CH₂SCF₃ H 0 B-2928 H H H H CH₃ CH₂SCHF₂ H 0 B-2929 H H H H CH₃ CH₂SCH₂CF₃ H 0 B-2930 H H H H CH₃ CH₂SCH₂CHF₂ H 0 B-2931 H H H H CH₃ CH₂SCF₂CF₃ H 0 B-2932 H H H H CH₃ CH₂CH₂SCF₃ H 0 B-2933 H H H H CH₃ CH₂CH₂SCH₂CF₃ H 0 B-2934 H H H H CH₃ CH₂CH₂CH₂SCF₃ H 0 B-2935 H H H H CH₃ CH₂CH₂CH₂SCH₂CF₃ H 0 B-2936 H H H H CH₃ CH(CH₃)SCF₃ H 0 B-2937 H H H H CH₃ CH(CH₃)SCH₂CF₃ H 0 B-2938 H H H H CH₃ CH₂CH(CH₃)SCF₃ H 0 B-2939 H H H H CH₃ CH₂CH(CH₃)SCH₂CF₃ H 0 B-2940 H H H H CH₃ CH(CH₃)CH₂CH₂SCF₃ H 0 B-2941 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₂CF₃ H 0 B-2942 H H H H CH₃ CH₂CH(CH₃)CH₂SCF₃ H 0 B-2943 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₂CF₃ H 0 B-2944 H H H H CH₃ CH₂CH₂CH(CH₃)SCF₃ H 0 B-2945 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₂CF₃ H 0 B-2946 H H H H CH₃ CH₂SOCF₃ H 0 B-2947 H H H H CH₃ CH₂CH₂SOCF₃ H 0 B-2948 H H H H CH₃ CH₂CH₂CH₂SOCF₃ H 0 B-2949 H H H H CH₃ CH(CH₃)SOCF₃ H 0 B-2950 H H H H CH₃ CH₂CH(CH₃)SOCF₃ H 0 B-2951 H H H H CH₃ CH(CH₃)CH₂CH₂SOCF₃ H 0 B-2952 H H H H CH₃ CH₂CH(CH₃)CH₂SOCF₃ H 0 B-2953 H H H H CH₃ CH₂CH₂CH(CH₃)SOCF₃ H 0 B-2954 H H H H CH₃ CH₂SO₂CF₃ H 0 B-2955 H H H H CH₃ CH₂CH₂SO₂CF₃ H 0 B-2956 H H H H CH₃ CH₂CH₂CH₂SO₂CF₃ H 0 B-2957 H H H H CH₃ CH(CH₃)SO₂CF₃ H 0 B-2958 H H H H CH₃ CH₂CH(CH₃)SO₂CF₃ H 0 B-2959 H H H H CH₃ CH(CH₃)CH₂CH₂SO₂CF₃ H 0 B-2960 H H H H CH₃ CH₂CH(CH₃)CH₂SO₂CF₃ H 0 B-2961 H H H H CH₃ CH₂CH₂CH(CH₃)SO₂CF₃ H 0 B-2962 H H H H CH₃ CH₂C(═O)CH₃ H 0 B-2963 H H H H CH₃ CH₂C(═O)CH₂CH₃ H 0 B-2964 H H H H CH₃ CH₂C(═O)C(CH₃)₃ H 0 B-2965 H H H H CH₃ CH₂CH₂C(═O)CH₃ H 0 B-2966 H H H H CH₃ CH₂CH₂C(═O)C(CH₃)₃ H 0 B-2967 H H H H CH₃ CH₂C(═C)CF₃ H 0 B-2968 H H H H CH₃ CH₂CH₂C(═O)CF₃ H 0 B 2969 H H H H CH₃ CH₂C(═O)OCH₃ H 0 B-2970 H H H H CH₃ CH₂C(═O)OCH₂CH₃ H 0 B-2971 H H H H CH₃ CH₂C(═O)OC(CH₃)₃ H 0 B-2972 H H H H CH₃ CH₂CH₂C(═O)OCH₃ H 0 B-2973 H H H H CH₃ CH₂CH₂C(═O)OCH₂CH₃ H 0 B-2974 H H H H CH₃ CH₂CH₂C(═O)OC(CH₃)₃ H 0 B-2975 H H H H CH₃ CH₂C(═O)NH₂ H 0 B-2976 H H H H CH₃ CH₂CH₂C(═O)NH₂ H 0 B-2977 H H H H CH₃ CH₂C(═O)NHCH₃ H 0 B-2978 H H H H CH₃ CH₂C(═O)NHCH(CH₃)₂ H 0 B-2979 H H H H CH₃ CH₂CH₂C(═O)NHCH₃ H 0 B-2980 H H H H CH₃ CH₂CH₂C(═O)NHCH(CH₃)₂ H 0 B-2981 H H H H CH₃ CH₂C(═O)NHCH₂CHF₂ H 0 B-2982 H H H H CH₃ CH₂C(═O)NHCH₂CF₃ H 0 B-2983 H H H H CH₃ CH₂CH₂C(═O)NHCH₂CHF₂ H 0 B-2984 H H H H CH₃ CH₂CH₂C(═O)NHCH₂CF₃ H 0

TABLE 143 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-2985 H H H H CH₃ CH₂C(═O)N(CH₃)₂ H 0 B-2986 H H H H CH₃ CH₂C(═O)N(CH₂CH₃)₂ H 0 B-2987 H H H H CH₃ CH₂CH₂C(═O)N(CH₃)₂ H 0 B-2988 H H H H CH₃ CH₂CH₂C(═O)N(CH₂CH₃)₂ H 0 B-2989 H H H H CH₃ CH₂CH₂OH H 0 B-2990 H H H H CH₃ CH₂CH(OH)CH₃ H 0 B-2991 H H H H CH₃ CH₂CH₂CH₂OH H 0 B-2992 H H H H CH₃ CH₂CH(OH)CH₂CH₃ H 0 B-2993 H H H H CH₃ CH₂CH(OH)C(CH₃)₃ H 0 B-2994 H H H H CH₃ CH₂CH₂CH(OH)CH₃ H 0 B-2995 H H H H CH₃ CH₂CH₂CH(OH)C(CH₃)₃ H 0 B-2996 H H H H CH₃ CH₂C(═NOH)CH₃ H 0 B-2997 H H H H CH₃ CH₂C(═NOH)CH₂CH₃ H 0 B-2998 H H H H CH₃ CH₂C(═NOH)C(CH₃)₃ H 0 B-2999 H H H H CH₃ CH₂C(═NOCH₃)CH₃ H 0 B-3000 H H H H CH₃ CH₂C(═NOCH₃)CH₂CH₃ H 0 B-3001 H H H H CH₃ CH₂C(═NOCH₂CH₃)CH₃ H 0 B-3002 H H H H CH₃ CH₂C(═NOCH₂CH₃)CH₂CH₃ H 0 B-3003 H H H H CH₃ CH₂C(═NOCH₂CF₃)CH₃ H 0 B-3004 H H H H CH₃ CH₂C(═NOCH₂CF₃)CH₂CH₃ H 0 B-3005 H H H H CH₃ CH₂Ph H 0 B-3006 H H H H CH₃ CH₂(2-F)Ph H 0 B-3007 H H H H CH₃ CH₂(3-F)Ph H 0 B-3008 H H H H CH₃ CH₂(4-F)Ph H 0 B-3009 H H H H CH₃ CH₂(2-Cl)Ph H 0 B-3010 H H H H CH₃ CH₂(3-Cl)Ph H 0 B-3011 H H H H CH₃ CH₂(4-Cl)Ph H 0 B-3012 H H H H CH₃ CH₂(2-CF₃)Ph H 0 B-3013 H H H H CH₃ CH₂(3-CF₃)Ph H 0 B-3014 H H H H CH₃ CH₂(4-CF₃)Ph H 0 B-3015 H H H H CH₃ CH₂(naphthalen-1-yl) H 0 B-3016 H H H H CH₃ CH₂(naphthalen-2-yl) H 0 B-3017 H H H H CH₃ CH₂CH₂Ph H 0 B-3018 H H H H CH₃ H CH₂CH₃ 0 B-3019 H H H H CH₃ CH₃ CH₂CH₃ 0 B-3020 H H H H CH₃ CH₂CH₃ CH₂CH₃ 0 B-3021 H H H H CH₃ CH(CH₃)₂ CH₂CH₃ 0 B-3022 H H H H CH₃ CH₂CH₂CH₃ CH₂CH₃ 0 B-3023 H H H H CH₃ CH₂CH(CH₃)₂ CH₂CH₃ 0 B-3024 H H H H CH₃ CH₂C(CH₃)₃ CH₂CH₃ 0 B-3025 H H H H CH₃ CH(CH₃)CH₂CH₃ CH₂CH₃ 0 B-3026 H H H H CH₃ CH₂(CH₂)₂CH₃ CH₂CH₃ 0 B-3027 H H H H CH₃ CH₂(CH₂)₃CH₃ CH₂CH₃ 0 B-3028 H H H H CH₃ CH₂(CH₂)₄CH₃ CH₂CH₃ 0 B-3029 H H H H CH₃ CH₂(CH₂)₆CH₃ CH₂CH₃ 0 B-3030 H H H H CH₃ CH₂OCH₃ CH₂CH₃ 0 B-3031 H H H H CH₃ CH₂OCH₂CH₃ CH₂CH₃ 0 B-3032 H H H H CH₃ CH₂CH₂OCH₃ CH₂CH₃ 0 B-3033 H H H H CH₃ CH₂CH₂OCH₂CH₃ CH₂CH₃ 0 B-3034 H H H H CH₃ CF₃ CH₂CH₃ 0 B-3035 H H H H CH₃ CHF₂ CH₂CH₃ 0 B-3036 H H H H CH₃ CH₂CF₃ CH₂CH₃ 0 B-3037 H H H H CH₃ CH₂CHF₂ CH₂CH₃ 0 B-3038 H H H H CH₃ CH₂CClF₂ CH₂CH₃ 0 B-3039 H H H H CH₃ CH₂CBrF₂ CH₂CH₃ 0 B-3040 H H H H CH₃ CF₂CF₃ CH₂CH₃ 0 B-3041 H H H H CH₃ CF₂CHF₂ CH₂CH₃ 0 B-3042 H H H H CH₃ CH₂CH₂CF₃ CH₂CH₃ 0 B-3043 H H H H CH₃ CH₂CF₂CF₃ CH₂CH₃ 0 B-3044 H H H H CH₃ CH₂CF₂CHF₂ CH₂CH₃ 0 B-3045 H H H H CH₃ CF₂CHFCF₃ CH₂CH₃ 0

TABLE 144 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-3046 H H H H CH₃ CF₂CF₂CF₃ CH₂CH₃ 0 B-3047 H H H H CH₃ CH₂CF₂CF₂CF₃ CH₂CH₃ 0 B-3048 H H H H CH₃ CH₂CF₂CHFCF₃ CH₂CH₃ 0 B-3049 H H H H CH₃ CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-3050 H H H H CH₃ CH₂CH₂CF₂CF₃ CH₂CH₃ 0 B-3051 H H H H CH₃ CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-3052 H H H H CH₃ CH₂CH₂CH(CF₃)₂ CH₂CH₃ 0 B-3053 H H H H CH₃ CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-3054 H H H H CH₃ CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0 B-3055 H H H H CH₃ CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-3056 H H H H CH₃ CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 0 B-3057 H H H H CH₃ CH₂CF₂CF(CF₃)CF₂C(CF₃)₃ CH₂CH₃ 0 B-3058 H H H H CH₃ CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-3059 H H H H CH₃ CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 0 B-3060 H H H H CH₃ CF₂CHFOCH₃ CH₂CH₃ 0 B-3061 H H H H CH₃ CF₂CHFOCH₂CH₃ CH₂CH₃ 0 B-3062 H H H H CH₃ CH₂CH₂OCH₂CF₃ CH₂CH₃ 0 B-3063 H H H H CH₃ CF₂CHFOCF₃ CH₂CH₃ 0 B-3064 H H H H CH₃ CF₂CHFOCF₂CF₃ CH₂CH₃ 0 B-3065 H H H H CH₃ CF₂CHFOCF₂CF₂CF₃ CH₂CH₃ 0 B-3066 H H H H CH₃ CH₂CH═CH₂ CH₂CH₃ 0 B-3067 H H H H CH₃ CH₂CH═CHCl CH₂CH₃ 0 B-3068 H H H H CH₃ CH₂CH═CCl₂ CH₂CH₃ 0 B-3069 H H H H CH₃ CH₂CH₂CF═CF₂ CH₂CH₃ 0 B-3070 H H H H CH₃ CH₂CH₂CH═CF₂ CH₂CH₃ 0 B-3071 H H H H CH₃ CH₂C≡CH CH₂CH₃ 0 B-3072 H H H H CH₃ CH₂C≡CCH₃ CH₂CH₃ 0 B-3073 H H H H CH₃ CH₂C≡Cl CH₂CH₃ 0 B-3074 H H H H CH₃ CH₂C≡CCF₃ CH₂CH₃ 0 B-3075 H H H H CH₃ cyclobutyl CH₂CH₃ 0 B-3076 H H H H CH₃ cyclopentyl CH₂CH₃ 0 B-3077 H H H H CH₃ cyclohexyl CH₂CH₃ 0 B-3078 H H H H CH₃ 4,4-difluorocyclohexyl CH₂CH₃ 0 B-3079 H H H H CH₃ CH₂(cyclopropyl) CH₂CH₃ 0 B-3080 H H H H CH₃ CH₂(cyclobutyl) CH₂CH₃ 0 B-3081 H H H H CH₃ CH₂(cyclopentyl) CH₂CH₃ 0 B-3082 H H H H CH₃ CH₂CH₂(cyclopropyl) CH₂CH₃ 0 B-3083 H H H H CH₃ CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-3084 H H H H CH₃ CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-3085 H H H H CH₃ CH₂(4,4-difluorocyclohexyl) CH₂CH₃ 0 B-3086 H H H H CH₃ CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 0 B-3087 H H H H CH₃ CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 0 B-3088 H H H H CH₃ CH₂SCH₃ CH₂CH₃ 0 B-3089 H H H H CH₃ CH₂SCH₂CH₃ CH₂CH₃ 0 B-3090 H H H H CH₃ CH₂CH₂SCH₃ CH₂CH₃ 0 B-3091 H H H H CH₃ CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-3092 H H H H CH₃ CH₂CH₂CH₂SCH₃ CH₂CH₃ 0 B-3093 H H H H CH₃ CH₂CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-3094 H H H H CH₃ CH(CH₃)SCH₃ CH₂CH₃ 0 B-3095 H H H H CH₃ CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-3096 H H H H CH₃ CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-3097 H H H H CH₃ CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-3098 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₃ CH₂CH₃ 0 B-3099 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₂CH₃ CH₂CH₃ 0 B-3100 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₃ CH₂CH₃ 0 B-3101 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₂CH₃ CH₂CH₃ 0 B-3102 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₃ CH₂CH₃ 0 B-3103 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₂CH₃ CH₂CH₃ 0 B-3104 H H H H CH₃ CH₂SOCH₃ CH₂CH₃ 0 B-3105 H H H H CH₃ CH₂CH₂SOCH₃ CH₂CH₃ 0 B-3106 H H H H CH₃ CH₂CH₂CH₂SOCH₃ CH₂CH₃ 0

TABLE 145 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-3107 H H H H CH₃ CH(CH₃)SOCH₃ CH₂CH₃ 0 B-3108 H H H H CH₃ CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-3109 H H H H CH₃ CH(CH₃)CH₂CH₂SOCH₃ CH₂CH₃ 0 B-3110 H H H H CH₃ CH₂CH(CH₃)CH₂SOCH₃ CH₂CH₃ 0 B-3111 H H H H CH₃ CH₂CH₂CH(CH₃)SOCH₃ CH₂CH₃ 0 B-3112 H H H H CH₃ CH₂SO₂CH₃ CH₂CH₃ 0 B-3113 H H H H CH₃ CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-3114 H H H H CH₃ CH₂CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-3115 H H H H CH₃ CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-3116 H H H H CH₃ CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-3117 H H H H CH₃ CH(CH₃)CH₂CH₂SO₂CH₃ CH₂CH₃ 0 B-3118 H H H H CH₃ CH₂CH(CH₃)CH₂SO₂CH₃ CH₂CH₃ 0 B-3119 H H H H CH₃ CH₂CH₂CH(CH₃)SO₂CH₃ CH₂CH₃ 0 B-3120 H H H H CH₃ CH₂SCF₃ CH₂CH₃ 0 B-3121 H H H H CH₃ CH₂SCHF₂ CH₂CH₃ 0 B-3122 H H H H CH₃ CH₂SCH₂CF₃ CH₂CH₃ 0 B-3123 H H H H CH₃ CH₂SCH₂CHF₂ CH₂CH₃ 0 B-3124 H H H H CH₃ CH₂SCF₂CF₃ CH₂CH₃ 0 B-3125 H H H H CH₃ CH₂CH₂SCF₃ CH₂CH₃ 0 B-3126 H H H H CH₃ CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-3127 H H H H CH₃ CH₂CH₂CH₂SCF₃ CH₂CH₃ 0 B-3128 H H H H CH₃ CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-3129 H H H H CH₃ CH(CH₃)SCF₃ CH₂CH₃ 0 B-3130 H H H H CH₃ CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-3131 H H H H CH₃ CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-3132 H H H H CH₃ CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-3133 H H H H CH₃ CH(CH₃)CH₂CH₂SCF₃ CH₂CH₃ 0 B-3134 H H H H CH₃ CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 0 B-3135 H H H H CH₃ CH₂CH(CH₃)CH₂SCF₃ CH₂CH₃ 0 B-3136 H H H H CH₃ CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 0 B-3137 H H H H CH₃ CH₂CH₂CH(CH₃)SCF₃ CH₂CH₃ 0 B-3138 H H H H CH₃ CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 0 B-3139 H H H H CH₃ CH₂SOCF₃ CH₂CH₃ 0 B-3140 H H H H CH₃ CH₂CH₂SOCF₃ CH₂CH₃ 0 B-3141 H H H H CH₃ CH₂CH₂CH₂SOCF₃ CH₂CH₃ 0 B-3142 H H H H CH₃ CH(CH₃)SOCF₃ CH₂CH₃ 0 B-3143 H H H H CH₃ CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-3144 H H H H CH₃ CH(CH₃)CH₂CH₂SOCF₃ CH₂CH₃ 0 B-3145 H H H H CH₃ CH₂CH(CH₃)CH₂SOCF₃ CH₂CH₃ 0 B-3146 H H H H CH₃ CH₂CH₂CH(CH₃)SOCF₃ CH₂CH₃ 0 B-3147 H H H H CH₃ CH₂SO₂CF₃ CH₂CH₃ 0 B-3148 H H H H CH₃ CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-3149 H H H H CH₃ CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-3150 H H H H CH₃ CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-3151 H H H H CH₃ CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-3152 H H H H CH₃ CH(CH₃)CH₂CH₂SO₂CF₃ CH₂CH₃ 0 B-3153 H H H H CH₃ CH₂CH(CH₃)CH₂SO₂CF₃ CH₂CH₃ 0 B-3154 H H H H CH₃ CH₂CH₂CH(CH₃)SO₂CF₃ CH₂CH₃ 0 B-3155 H H H H CH₃ CH₂C(═O)CH₃ CH₂CH₃ 0 B-3156 H H H H CH₃ CH₂C(═O)CH₂CH₃ CH₂CH₃ 0 B-3157 H H H H CH₃ CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-3158 H H H H CH₃ CH₂CH₂C(═O)CH₃ CH₂CH₃ 0 B-3159 H H H H CH₃ CH₂CH₂C(═O)C(CH₃)₃ CH₂CH₃ 0 B-3160 H H H H CH₃ CH₂C(═O)CF₃ CH₂CH₃ 0 B-3161 H H H H CH₃ CH₂CH₂C(═O)CF₃ CH₂CH₃ 0 B-3162 H H H H CH₃ CH₂C(═O)OCH₃ CH₂CH₃ 0 B-3163 H H H H CH₃ CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-3164 H H H H CH₃ CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0 B-3165 H H H H CH₃ CH₂CH₂C(═O)OCH₃ CH₂CH₃ 0 B-3166 H H H H CH₃ CH₂CH₂C(═O)OCH₂CH₃ CH₂CH₃ 0 B-3167 H H H H CH₃ CH₂CH₂C(═O)OC(CH₃)₃ CH₂CH₃ 0

TABLE 146 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-3168 H H H H CH₃ CH₂C(═O)NH₂ CH₂CH₃ 0 B-3169 H H H H CH₃ CH₂CH₂C(═O)NH₂ CH₂CH₃ 0 B-3170 H H H H CH₃ CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-3171 H H H H CH₃ CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-3172 H H H H CH₃ CH₂CH₂C(═O)NHCH₃ CH₂CH₃ 0 B-3173 H H H H CH₃ CH₂CH₂C(═O)NHCH(CH₃)₂ CH₂CH₃ 0 B-3174 H H H H CH₃ CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-3175 H H H H CH₃ CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-3176 H H H H CH₃ CH₂CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 0 B-3177 H H H H CH₃ CH₂CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 0 B-3178 H H H H CH₃ CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-3179 H H H H CH₃ CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-3180 H H H H CH₃ CH₂CH₂C(═O)N(CH₃)₂ CH₂CH₃ 0 B-3181 H H H H CH₃ CH₂CH₂C(═O)N(CH₂CH₃)₂ CH₂CH₃ 0 B-3182 H H H H CH₃ CH₂CH₂OH CH₂CH₃ 0 B-3183 H H H H CH₃ CH₂CH(OH)CH₃ CH₂CH₃ 0 B-3184 H H H H CH₃ CH₂CH₂CH₂OH CH₂CH₃ 0 B-3185 H H H H CH₃ CH₂CH(OH)CH₂CH₃ CH₂CH₃ 0 B-3186 H H H H CH₃ CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-3187 H H H H CH₃ CH₂CH₂CH(OH)CH₃ CH₂CH₃ 0 B-3188 H H H H CH₃ CH₂CH₂CH(OH)C(CH₃)₃ CH₂CH₃ 0 B-3189 H H H H CH₃ CH₂C(═NOH)CH₃ CH₂CH₃ 0 B-3190 H H H H CH₃ CH₂C(═NOH)CH₂CH₃ CH₂CH₃ 0 B-3191 H H H H CH₃ CH₂C(═NOH)C(CH₃)₃ CH₂CH₃ 0 B-3192 H H H H CH₃ CH₂C(═NOCH₃)CH₃ CH₂CH₃ 0 B-3193 H H H H CH₃ CH₂C(═NOCH₃)CH₂CH₃ CH₂CH₃ 0 B-3194 H H H H CH₃ CH₂C(═NOCH₂CH₃)CH₃ CH₂CH₃ 0 B-3195 H H H H CH₃ CH₂C(═NOCH₂CH₃)CH₂CH₃ CH₂CH₃ 0 B-3196 H H H H CH₃ CH₂C(═NOCH₂CF₃)CH₃ CH₂CH₃ 0 B-3197 H H H H CH₃ CH₂C(═NOCH₂CF₃)CH₂CH₃ CH₂CH₃ 0 B-3198 H H H H CH₃ CH₂Ph CH₂CH₃ 0 B-3199 H H H H CH₃ CH₂(2-F)Ph CH₂CH₃ 0 B-3200 H H H H CH₃ CH₂(3-F)Ph CH₂CH₃ 0 B-3201 H H H H CH₃ CH₂(4-F)Ph CH₂CH₃ 0 B-3202 H H H H CH₃ CH₂(2-Cl)Ph CH₂CH₃ 0 B-3203 H H H H CH₃ CH₂(3-Cl)Ph CH₂CH₃ 0 B-3204 H H H H CH₃ CH₂(4-Cl)Ph CH₂CH₃ 0 B-3205 H H H H CH₃ CH₂(2-CF₃)Ph CH₂CH₃ 0 B-3206 H H H H CH₃ CH₂(3-CF₃)Ph CH₂CH₃ 0 B-3207 H H H H CH₃ CH₂(4-CF₃)Ph CH₂CH₃ 0 B-3208 H H H H CH₃ CH₂(naphthalen-1-yl) CH₂CH₃ 0 B-3209 H H H H CH₃ CH₂(naphthalen-2-yl) CH₂CH₃ 0 B-3210 H H H H CH₃ CH₂CH₂Ph CH₂CH₃ 0 B-3211 H H H H H H H 1 B-3212 H H H H H CH₃ H 1 B-3213 H H H H H CH₂CH₃ H 1 B-3214 H H H H H CH(CH₃)₂ H 1 B-3215 H H H H H CH₂CH₂CH₃ H 1 B-3216 H H H H H CH₂CH(CH₃)₂ H 1 B-3217 H H H H H CH₂C(CH₃)₃ H 1 B-3218 H H H H H CH(CH₃)CH₂CH₃ H 1 B-3219 H H H H H CH₂(CH₂)₂CH₃ H 1 B-3220 H H H H H CH₂(CH₂)₃CH₃ H 1 B-3221 H H H H H CF₃ H 1 B-3222 H H H H H CHF₂ H 1 B-3223 H H H H H CH₂CF₃ H 1 B-3224 H H H H H CH₂CHF₂ H 1 B-3225 H H H H H CH₂CClF₂ H 1 B-3226 H H H H H CH₂CBrF₂ H 1 B-3227 H H H H H CF₂CF₃ H 1 B-3228 H H H H H CF₂CHF₂ H 1

TABLE 147 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-3229 H H H H H CH₂CH₂CF₃ H 1 B-3230 H H H H H CH₂CF₂CF₃ H 1 B-3231 H H H H H CH₂CF₂CHF₂ H 1 B-3232 H H H H H CF₂CHFCF₃ H 1 B-3233 H H H H H CF₂CF₂CF₃ H 1 B-3234 H H H H H CH₂CF₂CF₂CF₃ H 1 B-3235 H H H H H CH₂CF₂CHFCF₃ H 1 B-3236 H H H H H CH₂CH₂CH₂CF₃ H 1 B-3237 H H H H H CH₂CH₂CF₂CF₃ H 1 B-3238 H H H H H CF₂CF₂CF₂CF₃ H 1 B-3239 H H H H H CH₂CH₂CH(CF₃)₂ H 1 B-3240 H H H H H CF₂CF₂CF₂CF₂CF₃ H 1 B-3241 H H H H H CH₂CF₂CF₂CF₂CF₃ H 1 B-3242 H H H H H CH₂CH₂CH₂CH₂CF₃ H 1 B-3243 H H H H H CH₂CF₂CF₂CF₂CHF₂ H 1 B-3244 H H H H H CH₂CH₂CH₂CH₂CH₂CF₃ H 1 B-3245 H H H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ H 1 B-3246 H H H H H CH₂CH₂OCH₂CF₃ H 1 B-3247 H H H H H CF₂CHFOCF₃ H 1 B-3248 H H H H H CF₂CHFOCF₂CF₃ H 1 B-3249 H H H H H CH₂CH₂CF═CF₂ H 1 B-3250 H H H H H CH₂CH₂CH═CF₂ H 1 B-3251 H H H H H CH₂C≡CCH₃ H 1 B-3252 H H H H H CH₂C≡Cl H 1 B-3253 H H H H H CH₂C≡CCF₃ H 1 B-3254 H H H H H CH₂(2,2-difluorocyclopropyl) H 1 B-3255 H H H H H CH₂(2,2-dichlorocyclopropyl) H 1 B-3256 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) H 1 B-3257 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) H 1 B-3258 H H H H H CH₂SCH₃ H 1 B-3259 H H H H H CH₂SCH₂CH₃ H 1 B-3260 H H H H H CH₂CH₂SCH₃ H 1 B-3261 H H H H H CH₂SOCH₃ H 1 B-3262 H H H H H CH₂CH₂SOCH₃ H 1 B-3263 H H H H H CH₂SO₂CH₃ H 1 B-3264 H H H H H CH₂CH₂SO₂CH₃ H 1 B-3265 H H H H H CH₂SCF₃ H 1 B-3266 H H H H H CH₂SCHF₂ H 1 B-3267 H H H H H CH₂SCH₂CF₃ H 1 B-3268 H H H H H CH₂SCH₂CHF₂ H 1 B-3269 H H H H H CH₂SCF₂CF₃ H 1 B-3270 H H H H H CH₂CH₂SCF₃ H 1 B-3271 H H H H H CH₂CH₂SCH₂CF₃ H 1 B-3272 H H H H H CH₂CH₂CH₂SCH₂CF₃ H 1 B-3273 H H H H H CH(CH₃)SCH₂CF₃ H 1 B-3274 H H H H H CH₂CH(CH₃)SCH₂CF₃ H 1 B-3275 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ H 1 B-3276 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ H 1 B-3277 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ H 1 B-3278 H H H H H CH₂SOCF₃ H 1 B-3279 H H H H H CH₂CH₂SOCF₃ H 1 B-3280 H H H H H CH₂CH₂CH₂SOCF₃ H 1 B-3281 H H H H H CH₂SO₂CF₃ H 1 B-3282 H H H H H CH₂CH₂SO₂CF₃ H 1 B-3283 H H H H H CH₂CH₂CH₂SO₂CF₃ H 1 B-3284 H H H H H CH₂C(═O)NHCH₂CHF₂ H 1 B-3285 H H H H H CH₂C(═O)NHCH₂CF₃ H 1 B-3286 H H H H H H CH₂CH₃ 1 B-3287 H H H H H CH₃ CH₂CH₃ 1 B-3288 H H H H H CH₂CH₃ CH₂CH₃ 1 B-3289 H H H H H CH(CH₃)₂ CH₂CH₃ 1

TABLE 148 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-3290 H H H H H CH₂CH₂CH₃ CH₂CH₃ 1 B-3291 H H H H H CH₂CH(CH₃)₂ CH₂CH₃ 1 B-3292 H H H H H CH₂C(CH₃)₃ CH₂CH₃ 1 B-3293 H H H H H CH(CH₃)CH₂CH₃ CH₂CH₃ 1 B-3294 H H H H H CH₂(CH₂)₂CH₃ CH₂CH₃ 1 B-3295 H H H H H CH₂(CH₂)₃CH₃ CH₂CH₃ 1 B-3296 H H H H H CF₃ CH₂CH₃ 1 B-3297 H H H H H CHF₂ CH₂CH₃ 1 B-3298 H H H H H CH₂CF₃ CH₂CH₃ 1 B-3299 H H H H H CH₂CHF₂ CH₂CH₃ 1 B-3300 H H H H H CH₂CClF₂ CH₂CH₃ 1 B-3301 H H H H H CH₂CBrF₂ CH₂CH₃ 1 B-3302 H H H H H CF₂CF₃ CH₂CH₃ 1 B-3303 H H H H H CF₂CHF₂ CH₂CH₃ 1 B-3304 H H H H H CH₂CH₂CF₃ CH₂CH₃ 1 B-3305 H H H H H CH₂CF₂CF₃ CH₂CH₃ 1 B-3306 H H H H H CH₂CF₂CHF₂ CH₂CH₃ 1 B-3307 H H H H H CF₂CHFCF₃ CH₂CH₃ 1 B-3308 H H H H H CF₂CF₂CF₃ CH₂CH₃ 1 B-3309 H H H H H CH₂CF₂CF₂CF₃ CH₂CH₃ 1 B-3310 H H H H H CH₂CF₂CHFCF₃ CH₂CH₃ 1 B-3311 H H H H H CH₂CH₂CH₂CF₃ CH₂CH₃ 1 B-3312 H H H H H CH₂CH₂CF₂CF₃ CH₂CH₃ 1 B-3313 H H H H H CF₂CF₂CF₂CF₃ CH₂CH₃ 1 B-3314 H H H H H CH₂CH₂CH(CF₃)₂ CH₂CH₃ 1 B-3315 H H H H H CF₂CF₂CF₂CF₂CF₃ CH₂CH₃ 1 B-3316 H H H H H CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 1 B-3317 H H H H H CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 1 B-3318 H H H H H CH₂CF₂CF₂CF₂CHF₂ CH₂CH₃ 1 B-3319 H H H H H CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 1 B-3320 H H H H H CH₂CH₂CH₂CH₂CH₂CH₂CF₃ CH₂CH₃ 1 B-3321 H H H H H CH₂CH₂OCH₂CF₃ CH₂CH₃ 1 B-3322 H H H H H CF₂CHFOCF₃ CH₂CH₃ 1 B-3323 H H H H H CF₂CHFOCF₂CF₃ CH₂CH₃ 1 B-3324 H H H H H CH₂CH₂CF═CF₂ CH₂CH₃ 1 B-3325 H H H H H CH₂CH₂CH═CF₂ CH₂CH₃ 1 B-3326 H H H H H CH₂C≡CCH₃ CH₂CH₃ 1 B-3327 H H H H H CH₂C≡Cl CH₂CH₃ 1 B-3328 H H H H H CH₂C≡CCF₃ CH₂CH₃ 1 B-3329 H H H H H CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 1 B-3330 H H H H H CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 1 B-3331 H H H H H CH₂CH₂(2,2-difluorocyclopropyl) CH₂CH₃ 1 B-3332 H H H H H CH₂CH₂(2,2-dichlorocyclopropyl) CH₂CH₃ 1 B-3333 H H H H H CH₂SCH₃ CH₂CH₃ 1 B-3334 H H H H H CH₂SCH₂CH₃ CH₂CH₃ 1 B-3335 H H H H H CH₂CH₂SCH₃ CH₂CH₃ 1 B-3336 H H H H H CH₂SOCH₃ CH₂CH₃ 1 B-3337 H H H H H CH₂CH₂SOCH₃ CH₂CH₃ 1 B-3338 H H H H H CH₂SO₂CH₃ CH₂CH₃ 1 B-3339 H H H H H CH₂CH₂SO₂CH₃ CH₂CH₃ 1 B-3340 H H H H H CH₂SCF₃ CH₂CH₃ 1 B-3341 H H H H H CH₂SCHF₂ CH₂CH₃ 1 B-3342 H H H H H CH₂SCH₂CF₃ CH₂CH₃ 1 B-3343 H H H H H CH₂SCH₂CHF₂ CH₂CH₃ 1 B-3344 H H H H H CH₂SCF₂CF₃ CH₂CH₃ 1 B-3345 H H H H H CH₂CH₂SCF₃ CH₂CH₃ 1 B-3346 H H H H H CH-CH₂SCH₂CF₃ CH₂CH₃ 1 B-3347 H H H H H CH₂CH₂CH₂SCH₂CF₃ CH₂CH₃ 1 B-3348 H H H H H CH(CH₃)SCH₂CF₃ CH₂CH₃ 1 B-3349 H H H H H CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 1 B-3350 H H H H H CH(CH₃)CH₂CH₂SCH₂CF₃ CH₂CH₃ 1

TABLE 149 Compound R¹ R² R³ R⁴ R⁵ R⁶ R¹⁶ n B-3351 H H H H H CH₂CH(CH₃)CH₂SCH₂CF₃ CH₂CH₃ 1 B-3352 H H H H H CH₂CH₂CH(CH₃)SCH₂CF₃ CH₂CH₃ 1 B-3353 H H H H H CH₂SOCF₃ CH₂CH₃ 1 B-3354 H H H H H CH₂CH₂SOCF₃ CH₂CH₃ 1 B-3355 H H H H H CH₂CH₂CH₂SOCF₃ CH₂CH₃ 1 B-3356 H H H H H CH₂SO₂CF₃ CH₂CH₃ 1 B-3357 H H H H H CH₂CH₂SO₂CF₃ CH₂CH₃ 1 B-3358 H H H H H CH₂CH₂CH₂SO₂CF₃ CH₂CH₃ 1 B-3359 H H H H H CH₂C(═O)NHCH₂CHF₂ CH₂CH₃ 1 B-3360 H H H H H CH₂C(═O)NHCH₂CF₃ CH₂CH₃ 1 B-3361 H H H H H CH₂CH₂CF₂CF₂CF₂CF₃ CH₂CH₃ 0

On the other hand, the present compound represented by general formula [I] or [II] can be produced in accordance with, but not limited to, the production methods shown below. Hereinafter, for example, “compound represented by general formula [I]” is synonymous to “compound represented by formula [I]” and “compound [I]”.

<Production Method 1>

A compound represented by general formula [V] among the present compounds can be produced, for example, in accordance with the following method.

(wherein, R¹⁷ represents a C₁-C₆ alkyl group, and R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined above.)

That is, the compound represented by general formula [V] can be produced by reacting the compound represented by general formula [III] and the compound represented by general formula [IV] in an appropriate solvent in the presence or absence of an appropriate base.

The use amount of compound [IV] used in the present reaction may be appropriately selected from the range of typically 1 to 500 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [III].

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, methyltert-butylether, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2-dichloroethane; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, or 2-propanol; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate or ethyl propionate; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine or picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.2 to 50 liters relative to 1 mol of compound [III].

Examples of the base that can be used in the present reaction include inorganic bases including: hydroxides of alkali metal such as sodium hydroxide or potassium hydroxide; hydroxides of alkali earth metal such as calcium hydroxide or magnesium hydroxide; carbonates of alkali metal such as sodium carbonate or potassium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; or organic bases including: metal hydrides such as sodium hydride or potassium hydride; metal salts of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; or triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminopyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 0 to 5 mol, and is preferably 0 to 1.2 mol, relative to 1 mol of compound [II].

The reaction temperature of the present reaction may be selected from any range of temperature typically from −30° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [V] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. The isolated compound [V] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 2>

A compound represented by general formula [VI] among the present compounds can be produced, for example, in accordance with the following method.

(wherein, R¹, R², R³, R⁴, R⁵, R⁶, and R¹⁷ are as defined above.)

That is, the compound represented by general formula [VI] can be produced by hydrolysis of compound [III] in an appropriate solvent in the presence of an appropriate base or appropriate acid.

Examples of the base that can be used in the present reaction include inorganic bases including hydroxides of alkali metal such as sodium hydroxide, potassium hydroxide, lithium hydroxide, or barium hydroxide; carbonates of alkali metal such as sodium carbonate or potassium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate. The use amount of the base may be appropriately selected from the range of 0.1 to 50 mol, and is preferably 0.5 to 20 mol, relative to 1 mol of compound [III].

Examples of the acid that can be used in the present reaction include inorganic acids such as hydrochloric acid, hydrobromic acid, or sulfuric acid; or carboxylic acids such as acetic acid or trifluoroacetic acid. The use amount of the acid may be appropriately selected from the range of 1 to 1000 mol, and is preferably 1 to 100 mol, relative to 1 mol of compound [III].

Examples of the solvent that can be used in the present reaction include ethers such as diethyl ether, tetrahydrofuran, methyl tert-butyl ether, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, or 2-propanol; nitriles such as acetonitrile or propionitrile; ketones such as acetone or methylethylketone; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.3 to 30 liters relative to 1 mol of compound [III].

The reaction temperature of the present reaction may be selected from any range of temperature typically from −30° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [VI] can be isolated by conducting an operation of pouring the reaction mixture into water and neutralizing the reaction mixture, and then collecting the precipitated solid by filtration or extracting with an organic solvent followed by concentration or the like operation. The isolated compound [VI] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 3>

A compound represented by general formula [V] among the present compounds can also be produced, for example, in accordance with the following method.

(wherein, X¹ represents a halogen atom, and R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined above.)

That is, the compound represented by general formula [V] can be produced by (step 1) making compound [VI] into compound [VII] by using an acid halogenating agent in an appropriate solvent in the presence or absence of an appropriate catalyst, and then (step 2) reacting with compound [IV] in an appropriate solvent in the presence or absence of an appropriate base.

(Step 1)

Examples of the acid halogenating agent that can be used in the present reaction include thionyl chloride, oxalyl chloride, or phosphoryl chloride. The use amount of the acid halogenating agent may be appropriately selected from the range of 0.1 to 30 mol, and is preferably 0.5 to 6 mol, relative to 1 mol of compound [VI].

Examples of the acid catalyst that can be used in the present reaction include N,N-dimethylformamide. The use amount of the catalyst may be appropriately selected from the range of 0.01 to 1 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of compound [VI].

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2-dichloroethane; nitriles such as acetonitrile or propionitrile; esters such as ethyl acetate, butyl acetate, or ethyl propionate; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; or mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to 10 liters relative to 1 mol of compound [VI].

The reaction temperature of the present reaction may be selected from any range of temperature typically from −30° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [VII] can be isolated by conducting concentration or the like operation.

(Step 2)

The use amount of compound [IV] used in the present reaction may be appropriately selected from the range of typically 1 to 500 mol, and is preferably 1.0 to 300 mol, relative to 1 mol of compound [VI].

The base, solvent, reaction temperature, and reaction time that can be used in the present reaction are as described in the Production method 1

After end of the reaction, compound [V] can be isolated by conducting an operation of pouring the reaction mixture into water, and then collecting the precipitated solid by filtration or extracting with an organic solvent followed by concentration or the like. The isolated compound [V] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 4>

A compound represented by general formula [V] among the present compounds can also be produced, for example, in accordance with the following method.

(wherein, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined above.)

That is, the compound represented by general formula [V] can be produced by reacting compound [VI] and compound [IV] in an appropriate solvent in the presence or absence of an appropriate condensing agent and an appropriate base.

The use amount of compound [IV] used in the present reaction may be appropriately selected from the range of 1 to 3 mol, and is preferably 1.0 to 1.2 mol, relative to 1 mol of compound [VI].

Examples of the condensing agent that can be used in the present reaction include 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride, 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide, N,N′-dicyclohexylcarbodiimide, N,N′-diisopropylcarbodiimide, N,N′-carbonyldiimidazole, 4-(4,6-dimethoxy-1,3,5-triazine-2-yl)-4-methylmorpholinium chloride, 1H-benzotriazole-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate, {{[(1-cyano-2-ethoxy-2-oxoethylidene)amino]oxy}-4-morpholinomethylene}dimethylammonium hexafluorophosphate, or O-(7-azabenzotriazole-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorofluorophosphate. The use amount of the condensing agent may be appropriately selected from the range of 1 to 3 mol, and is preferably 1.0 to 1.2 mol, relative to 1 mol of compound [VI].

When a base is used in the present reaction, examples of the base that can be used include organic bases such as triethylamine, 4-methylmorpholine, diisopropylethylamine, 1,8-diazabicyclo[5.4.0]-7-undecene, pyridine, 4-N,N-dimethylaminopyridine, or 2,6-lutidine. The use amount of the base may be appropriately selected from the range of 0 to 5 mol, and is preferably 0.1 to 2.2 mol, relative to 1 mol of compound [VI].

Examples of the solvent that can be used in the present reaction include halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2-dichloroethane; hydrocarbons such as hexane or heptane; esters such as ethyl acetate; nitriles such as acetonitrile or propionitrile; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; ethers such as diethylether, cyclopentylmethylether, tetrahydrofuran, 2-methyltetrahydrofuran, or 1,4-dioxane; or mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [VI].

The present reaction can be conducted in the presence of a catalyst as necessary, and examples of the catalyst include 4-(N,N-dimethyl)aminopyridine, or 4-hydroxybenzotriazole. The use amount of the catalyst may be appropriately selected from the range of 0.001 to 1 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of compound [VI].

The reaction temperature of the present reaction may be selected from any range of temperature from −20° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 80° C.

The reaction time of the present reaction is typically 1 minute to 48 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [V] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. The isolated compound [V] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 5>

A compound represented by general formula [IX] among the present compounds can be produced, for example, by using a compound represented by general formula [VIII] in accordance with the following method.

(wherein, R¹⁸ represents a group OR¹⁷ or a group NR⁷R⁸, R¹⁹ represents a benzyl group that is unsubstituted or substituted with R⁹, and R¹, R², R³, R⁴, R⁵, and R⁹ are as defined above.)

That is, the compound represented by general formula [IX] can be produced by hydrogenolysis reaction of a compound [VIII] in a hydrogen gas atmosphere, in an appropriate solvent in the presence of an appropriate catalyst.

Examples of the catalyst that is used in the present reaction include platinum, Raney nickel, platinum black, palladium-carbon, palladium black, palladium hydroxide-carbon, and platinum oxide. The use amount of the catalyst may be appropriately selected from the range of 0.01 to 1 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of compound [VIII].

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; ketones such as acetone, or 2-butanone; esters such as ethyl acetate, butyl acetate, or ethyl propionate; water, acetic acid, or mixed solvents thereof. The use amount of the solvent is 0.1 to 100 liters, preferably 0.3 to 30 liters relative to 1 mol of compound [VIII].

The reaction temperature of the present reaction may be selected from any range of temperature typically from 0° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [IX] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. Alternatively, compound [IX] can also be isolated by concentrating the solvent after filtering insoluble matters from the reaction mixture. The isolated compound [IX] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 6>

A compound represented by general formula [XII] among the present compounds can be produced, for example, by using a compound represented by general formula [IX] in accordance with the following method.

(wherein, R²⁰ represents a fluorine atom, C₁-C₆ alkoxy group, C₁-C₆ haloalkyl group, or C₁-C₆ haloalkoxy group, R¹, R², R³, R⁴, R⁵, R⁶, and R¹⁸ are as defined above, X² represents a halogen atom, C₁-C₆ alkylsulfonyloxy group, trifluoromethanesulfonyloxy group, nonafluorobutylsulfonyloxy group, phenylsulfonyloxy group, 4-toluenesulfonyloxy group, C₁-C₆ alkylsulfonyl group, phenylsulfonyl group, or 4-toluenesulfonyl group.)

That is, the compound represented by general formula [XII] can be produced by reacting compound [IX] and compound [X] or compound [XI] in an appropriate solvent in the presence or absence of an appropriate base.

The use amount of compound [X] or compound [XI] used in the present reaction may be appropriately selected from the range of 1 to 5 mol, and is preferably 1.0 to 1.2 mol, relative to 1 mol of compound [IX].

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile, or propionitrile; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine, or picoline; tertiary amines such as triethylamine, or tributylamine; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [IX].

Examples of the base that can be used in the present reaction include inorganic bases including: hydroxides of alkali metal such as sodium hydroxide or potassium hydroxide; hydroxides of alkali earth metal such as calcium hydroxide or magnesium hydroxide; carbonates of alkali metal such as sodium carbonate or potassium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; or organic bases including: metal hydrides such as sodium hydride or potassium hydride; metal salts of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; or triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminopyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 1 to 5 mol, and is preferably 1.0 to 1.2 mol, relative to 1 mol of compound [IX]. The organic bases such as triethylamine or pyridine can also be used as the solvent.

The reaction temperature of the present reaction may be selected from any range of temperature typically from −70° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [XII] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. The isolated compound [XII] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 7>

A compound represented by general formula [XII] among the present compounds can be produced, for example, by using a compound represented by general formula [IX] in accordance with the following method.

(wherein, R¹, R², R³, R⁴, R⁵, R⁶, and R¹⁸ are as defined above.)

That is, the compound represented by general formula [XII] can be produced by reacting compound [IX] and compound [XIII] in an appropriate solvent in the presence of trisubstituted phosphine and an azodicarboxylic acid derivative or in the presence of a phosphorane reagent.

The use amount of compound [XIII] used in the present reaction may be appropriately selected from the range of 1.0 to 5.0 mol, and is preferably 1.0 to 2.0 mol, relative to 1 mol of compound [IX].

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; nitriles such as acetonitrile, or propionitrile; halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2-dichloroethane; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; ketones such as acetone, methylethylketone, or cyclohexane; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [IX].

Examples of the trisubstituted phosphine that can be used in the present reaction include triphenylphosphine, tributylphosphine, or trimethylphosphine. The use amount of the trisubstituted phosphine may be appropriately selected from the range of 1.0 to 5.0 mol, and is preferably 1.0 to 3.0 mol, relative to 1 mol of compound [IX].

Examples of the azodicarboxylic acid derivative that can be used in the present reaction include diethyl azodicarboxylate, diisopropyl azodicarboxylate, dimethoxyethyl azodicarboxylate, or N,N,N′,N′,-tetramethyl azodicarboxylic amide. The use amount of the azodicarboxylic acid derivative may be appropriately selected from the range of 1.0 to 5.0 mol, and is preferably 1.0 to 2.0 mol, relative to 1 mol of compound [IX].

Examples of the phosphorane reagent that can be used in the present reaction include cyanomethylenetrimethylphosphorane, or cyanomethylenetributylphosphorane. The use amount of the phosphorane may be appropriately selected from the range of 1.0 to 5.0 mol, and is preferably 1.0 to 2.0 mol, relative to 1 mol of compound [IX]. The reaction temperature of the present reaction may be selected from any range of temperature typically from −30° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, reaction substrate, reaction amount and so on.

After end of the reaction, compound [XII] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. Compound [XII] can also be isolated by concentrating the solvent from the reaction mixture. The isolated compound [XII] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 8>

A compound represented by general formula [V] among the present compounds can be produced, for example, by using a compound represented by general formula [XIV] in accordance with the following method.

(wherein, X³ represents a halogen atom, C₁-C₆ alkylsulfonyloxy group, trifluoromethanesulfonyloxy group, nonafluorobutylsulfonyloxy group, phenylsulfonyloxy group, 4-toluenesulfonyloxy group, C₁-C₆ alkylsulfonyl group, phenylsulfonyl group, or 4-toluenesulfonyl group, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined above.) That is, the compound represented by general formula [V] can be produced by reacting compound [XIV] and compound [XV] or compound [XVI] in an appropriate solvent in the presence or absence of an appropriate base.

The use amount of compound [XV] or compound [XVI] used in the present reaction may be appropriately selected from the range of 1 to 10 mol, and is preferably 1.0 to 5.0 mol, relative to 1 mol of compound [XIV].

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, or sulfolane; alcohols such as methanol, ethanol, 2-propanol, or methyl cellosolve; nitriles such as acetonitrile, or propionitrile; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; pyridines such as pyridine, or picoline; water, or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [XIV].

Examples of the base that can be used in the present reaction include inorganic bases including: hydroxides of alkali metal such as sodium hydroxide or potassium hydroxide; hydroxides of alkali earth metal such as calcium hydroxide or magnesium hydroxide; carbonates of alkali metal such as sodium carbonate or potassium carbonate; bicarbonates of alkali metal such as sodium hydrogen carbonate or potassium hydrogen carbonate; or organic bases including: metal hydrides such as sodium hydride or potassium hydride; metal salts of alcohol such as sodium methoxide, sodium ethoxide, or potassium tert-butoxide; or triethylamine, N,N-dimethylaniline, pyridine, 4-N,N-dimethylaminopyridine, 1,8-diazacyclo[5.4.0]-7-undecene, and so on. The use amount of the base may be appropriately selected from the range of 1 to 10 mol, and is preferably 1 to 6 mol, relative to 1 mol of compound [XIV]. The organic bases such as triethylamine or pyridine can also be used as the solvent.

The present reaction can be conducted in the presence of a catalyst as necessary, and examples of the catalyst include pyridine, 4-(N,N-dimethyl)aminopyridine, or 4-pyrrolidinopyridine. The use amount of the catalyst may be appropriately selected from the range of 0.001 to 1 mol, and is preferably 0.01 to 0.1 mol, relative to 1 mol of compound [XIV].

The reaction temperature of the present reaction may be selected from any range of temperature typically from −70° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [V] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. The isolated compound [V] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 9>

A compound represented by general formula [XVII] among the present compounds can be produced, for example, by using a compound represented by general formula [V] in accordance with the following method.

(wherein, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined above.) That is, the compound represented by general formula [XVII] can be produced by reacting compound [V] and an appropriate sulfidizing agent.

Examples of the solvent that can be used in the present reaction include ethers such as diethylether, tetrahydrofuran, or 1,4-dioxane; aromatic hydrocarbons such as benzene, toluene, xylene, or chlorobenzene; aprotic polar solvents such as dimethylsulfoxide, or sulfolane, halogenated hydrocarbons such as dichloromethane, chloroform, or 1,2-dichloroethane; aliphatic hydrocarbons such as pentane, hexane, cyclohexane, or heptane; water or mixed solvents thereof. The use amount of the solvent is 0.1 to 300 liters, preferably 0.3 to 50 liters relative to 1 mol of compound [V].

Examples of the sulfidizing agent that can be used in the present reaction include phosphorus pentasulfide, and a Lawesson's reagent. The use amount of the sulfidizing agent may be appropriately selected from the range of 0.5 to 30 mol, and is preferably 0.5 to 5 mol, relative to 1 mol of compound [V].

The reaction temperature of the present reaction may be selected from any range of temperature typically from −70° C. to a reflux temperature in a reaction system, and is preferably in the range of 0° C. to 150° C.

The reaction time of the present reaction is typically 10 minutes to 24 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [XVII] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. Alternatively, compound [XVII] can also be isolated by concentrating the solvent of the reaction mixture. The isolated compound [XVII] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Production Method 10>

A compound represented by general formula [XIX] among the present compounds can be produced, for example, by using a compound represented by general formula [XVIII] in accordance with the following method.

(R²¹ represents a hydroxy group, group OR¹⁷, or group NR⁷R⁸, and wherein R¹, R², R³, R⁴, R⁵, and R⁶ are as defined above.) That is, the compound represented by general formula [XIX] can be produced by reacting compound [XVIII] and an appropriate oxidizing agent in an appropriate solvent in the presence or absence of a catalyst.

Examples of the solvent that can be used in the present reaction include halogenated hydrocarbons such as dichloromethane, chloroform, 1,2-dichloroethane, carbon tetrachloride, chlorobenzene, or dichlorobenzene; ethers such as 1,4-dioxane, tetrahydrofuran, 1,2-dimethoxyethane, or diethylether; amides such as N,N-dimethylacetamide, N,N-dimethylformamide, or N-methyl-2-pyrrolidinone; alcohols such as methanol, ethanol, propanol, isopropanol, butanol, or tert-butanol; ketones such as acetone or 2-butanone; nitriles such as acetonitrile or propionitrile; acetic acid, water, or mixtures thereof. The use amount of the solvent is 0.1 to 500 liters, preferably 0.3 to 200 liters relative to 1 mol of compound [XVIII].

Examples of the oxidizing agent include organic peroxides such as m-chloroperbenzoic acid, performic acid, or peracetic acid; and inorganic peroxides such as hydrogen peroxide, potassium permanganate, OXONE (registered tradename available from E. I. Du Pont de Nemours and Company, product containing potassium peroxymonosulfate), or sodium periodate. The use amount of the oxidizing agent is 0.5 to 3 mol, relative to 1 mol of compound [XVIII].

Examples of the catalyst that can be used in the present reaction include sodium tungstate. The use amount of the catalyst is 0.01 to 0.5 mol, relative to 1 mol of compound [XVIII].

The reaction temperature of the present reaction may be selected from any range of temperature typically from −30° C. to a reflux temperature in a reaction system, and is preferably in the range of −10° C. to 100° C.

The reaction time of the present reaction is typically 10 minutes to 48 hours although it differs depending on the reaction temperature, the reaction substrate, the reaction amount, and the like.

After end of the reaction, compound [XIX] can be isolated by conducting an operation of pouring the reaction mixture into water, and extracting with an organic solvent followed concentration or the like. Alternatively, compound [XIX] can also be isolated by concentrating the solvent of the reaction mixture. The isolated compound [XIX] can be further purified by column chromatography, recrystallization, or the like as necessary.

<Method for Producing Intermediate>

A compound represented by general formula [XXIII] can be produced, for example, by using a compound represented by general formula [XX] in accordance with the following method.

(wherein, R¹, R², R³, R⁴, R⁵, R¹⁷, and X¹ are as defined above.)

That is, the compound represented by general formula [XXIII] can be obtained by cyclization reaction after obtaining compound [XXII] by Japp-klingemann reaction between compound [XX] and compound [XXI]. The compound represented by general formula [XXIII] can be produced by a method described in WO 2012/028332 A, WO 2014/114649 A, WO 2016/027790 A, WO 2016/166250 A, or U.S. Pat. No. 5,055,482, or produced in accordance with such a method.

The present harmful organism control agent contains the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof represented by general formula [I] of the present invention, as an active ingredient. The present harmful organism control agent is representatively an insecticide and a miticide.

The present harmful organism control agent can contain an additive component (carrier) that is typically used in a pesticide formulation, as necessary. Also the pesticide composition can contain an additive component (carrier) that is typically used in a pesticide formulation.

Examples of the additive component include a carrier such as a solid carrier or a liquid carrier, a surfactant, a binder or a tackifier, a thickener, a coloring agent, a spreader, a sticker, an antifreezing agent, an anticaking agent, a disintegrating agent, and a stabilizing agent, and besides the above, an antiseptic, a plant piece, or the like may be added to the additive component as necessary. These additive components may be used singly or in combination of two or more kinds.

Hereinafter, the aforementioned additive components are described.

Examples of the solid carrier include mineral carriers such as pyrophyllite clay, kaolin clay, silica clay, talc, diatomite, zeolite, bentonite, Japanese acid clay, activated clay, attapulgus clay, vermiculite, pearlite, pumice, white carbon (synthetic silicic acid, synthetic silicate, or the like), or titanium dioxide; vegetal carriers such as woody powder, corn haulm, walnut shell, fruit stone, chaff, sawdust, bran, soybean meal, powdered cellulose, starch, dextrin, or saccgarudes; inorganic salt carriers such as calcium carbonate, ammonium sulfate, sodium sulfate, or potassium chloride; and polymeric carriers such as polyethylene, polypropylene, polyvinyl chloride, polyvinyl acetate, ethylene-vinyl acetate copolymer, or urea-aldehyde resin.

Examples of the liquid carrier include monohydric alcohols such as methanol, ethanol, propanol, isopropanol, butanol, or cyclohexanol; polyhydric alcohols such as ethylene glycol, diethylene glycol, propylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, or glycerin; polyhydric alcohol derivatives such as polypropylene glycol ether; ketones such as acetone, methylethyl ketone, methylisobutyl ketone, diisobutyl ketone, cyclohexanone, or isophoron; ethers such as ethyl ether, dioxane, Cellosolve, dipropyl ether, or tetrahydrofuran; aliphatic hydrocarbons such as normal paraffin, naphthene, isoparaffin, kerosene, or mineral oil; aromatic hydrocarbons such as toluene, C₉-C₁₀ alkylbenzene, xylene, solvent naphtha, alkyl naphthalene, or high boiling point aromatic hydrocarbons; halogenated hydrocarbons such as 1,2-dichloroethane, chloroform, or carbon tetrachloride; esters such as ethyl acetate, diisopropyl phthalate, dibutyl phthalate, dioctyl phthalate, or dimethyl adipate; lactones such as γ-butyrolactone; amides such as N,N-dimethylformamide, N,N-diethylformamide, N,N-dimethylacetamide, or N-alkylpyrrolidinone; nitriles such as acetonitrile; sulfur compounds such as dimethyl sulfoxide; vegetable oils such as soybean oil, rapeseed oil, cottonseed oil, coconut oil, or castor oil; and water.

Although not particularly limited, the surfactant preferably gelates or shows swelling property in water, and examples of the surfactant include nonionic surfactants such as sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sucrose fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene resin acid ester, polyoxyethylene fatty acid diester, polyoxyethylene alkyl ether, polyoxyethylene alkylphenyl ether, polyoxyethylene dialkylphenyl ether, polyoxyethylene alkylphenyl ether formalin condensate, polyoxyethylene polyoxypropylene block polymer, alkylpolyoxyethylene polypropylene block polymer ether, polyoxyethylene alkyl amine, polyoxyethylene fatty acid amide, polyoxyethylene fatty acid bisphenyl ether, polyalkylene benzyl phenyl ether, polyoxyalkylene styryl phenyl ether, acetylene diol, polyoxyalkylene-added acetylene diol, polyoxyethylene ether silicone, ester silicone, fluorine surfactant, polyoxyethylene castor oil, or polyoxyethylene hardened castor oil; anionic surfactants such as alkyl sulfates, polyoxyethylene alkyl ether sulfates, polyoxyethylene alkyl phenyl ether sulfates, polyoxyethylene styryl phenyl ether sulfate, alkyl benzenesulfonates, lignin sulfonate, alkyl sulfosuccinates, naphthalene sulfonate, alkylnaphthalene sulfonates, salts of formalin condensate of naphthalene sulfonate, fatty acid salts, polycarboxylates, N-methyl-fatty acid Sarcosinates, resinates, polyoxyethylene alkyl ether phosphates, or polyoxyethylene alkyl phenylether phosphates; cationic surfactants such as alkyl amine salts such as lauryl amine hydrochloride, stearyl amine hydrochloride, oleyl amine hydrochloride, stearyl amine acetate, stearyl aminopropylamine acetate, alkyl trimethyl ammonium chlorides, or alkyl dimethylbenzarconium chloride; and amphoteric surfactants including a betaine type such as dialkyl diaminoethyl betaine, or alkyl dimethylbenzyl betaine, and an amino acid type such as dialkylaminoethyl glycin, or alkyl dimethylbenzyl glycin.

Examples of the binder or the tackifier include carboxymethylcelullose or a salt thereof, dextrin, soluble starch, xanthan gum, guar gum, sucrose, polyvinylpyrrolidone, gum arabic, polyvinyl alcohol, polyvinyl acetate, sodium polyacrylate, polyethylene glycol having an average molecular weight of 6000 to 20000, polyethylene oxide having an average molecular weight of 100000 to 5000000, and naturally-occurring phospholipid (for example, Cephalin acid, lecithin, or the like).

Examples of the thickener include water-soluble polymers such as xanthan gum, guar gum, carboxymethylcelullose, polyvinylpyrrolidone, carboxyvinyl polymer, acrylic polymer, starch derivatives, or polysaccharides; and inorganic fine powder such as high purity bentonite or white carbon.

Examples of the coloring agent include inorganic pigments such as iron oxide, titanium oxide, or Prussian blue; and organic dyes such as an alizarin dye, an azo dye, or a metal phthalocyanine dye.

Examples of the spreader include a silicone surfactant, cellulose powder, dextrin, processed starch, a polyaminocarboxylic acid chelate compound, a cross-linked polyvinylpyrrolidone, malic acid and styrenes, methacrylic acid copolymer, a half ester of a polymer of polyhydric alcohol and dicarboxylic acid anhydride, and a water-soluble salt of polystyrene sulfonic acid.

Examples of the sticker include various surfactants such as sodium dialkyl sulfosuccinate, polyoxyethylene alkyl ether, polyoxyethylene alkylphenyl ether, or polyoxyethylene fatty acid ester; paraffin, terpene, polyamide resin, polyacrylate, polyoxyethylene, wax, polyvinylalkyl ether, an alkylphenol formalin condensate, and a synthetic resin emulsion.

Examples of the antifreezing agent include polyhydric alcohols such as ethylene glycol, diethylene glycol, propylene glycol, or glycerin.

Examples of the anticaking agent include polysaccharides such as starch, alginic acid, mannose, or galactose; polyvinylpyrrolidone, white carbon, ester gum, and petroleum resin.

Examples of the disintegrating agent include sodium tripolyphosphate, sodium hexametaphosphate, a stearic metal salt, cellulose powder, dextrin, copolymer of methacrylic ester, polyvinylpyrrolidone, polyaminocarboxylic chelate compound, styrene sulfonate-isobutylene-maleic anhydride copolymer, and starch-polyacrylonitrile graft copolymer.

Examples of the stabilizing agent include a desiccant such as zeolite, calcined lime, or magnesium oxide; an antioxidant based on phenol, amine, sulfur, phosphoric acid, or the like; an ultraviolet absorber based on salicylic acid, benzophenone, or the like.

In the present harmful organism control agent, when the additive component is contained, the content thereof is selected typically in a range of 5 to 95%, preferably in the range of 20 to 90% on the mass basis in the case of a carrier such as a solid carrier or a liquid carrier, typically in a range of 0.1% to 30%, preferably in a range of 0.5 to 10% in the case of a surfactant, and typically in a range of 0.1 to 30%, preferably in a range of 0.5 to 10% in the case of other additive.

The present harmful organism control agent is used while it is prepared into any formulation including dusts, dusts and granules, granules, water-dispersible powders, water-soluble powders, water-dispersible granules, tablets, Jumbos, emulsifiable concentrates, oils, solutions, flowable concentrates, emulsions, microemulsions, suspoemulsions, ultra-low volume formulations, microcapsules, smoking agents, aerosols, baiting agents, and pastes.

In actual use of the formulation, the formulation can be used per se or after dilution with a diluent such as water in a predetermined concentration. Application of various formulations containing the present compound, and dilution products thereof can be conducted by a method ordinarily used, such as dispersion (e.g., spraying, misting, atomizing, powder dispersion, granule dispersion, on-water-surface dispersion, or inbox dispersion), in-soil application (e.g., mixing or drenching), on-surface application (e.g., coating, dust coating, or covering), seed treatment (e.g., smearing or dressing treatment), immersion, poison bait, smoking, and the like. It is also possible to mix the above-mentioned active ingredient with a livestock feed in order to prevent the infestation and growth of pests, particularly harmful insects in the excreta of the livestock.

A method for controlling a harmful organism of the present invention can be conducted by using an active ingredient amount of the compound represented by general formula [I] of the present invention or a salt thereof in the above-mentioned application method described above.

The mixing proportion (% by mass) of the active ingredient in the present harmful organism control agent is appropriately selected as needed. For example, the mixing proportion may be appropriately selected typically in a range of 0.01 to 20%, preferably 0.05 to 10% for dusts, dusts and granules, microgranules, or the like; typically in a range of 0.1 to 30%, preferably 0.5 to 20% for granules or the like; typically in a range of 1 to 70%, preferably 5 to 50% for water-dispersible powders, water-dispersible granules, or the like; typically in a range of 1 to 95%, preferably 10 to 80% for water-soluble powders, solutions, or the like; typically in a range of 5 to 90%, preferably 10 to 80% for emulsifiable concentrates or the like; typically in a range of 1 to 50%, preferably 5 to 30% for oils or the like; typically in a range of 5 to 60%, preferably 10 to 50% for flowable concentrates or the like; typically in a range of 5 to 70%, preferably 10 to 60% for emulsions, microemulsions, suspoemulsions, or the like; typically in a range of 1 to 80%, preferably 5 to 50% for tablets, baiting agents, pastes, or the like; typically in a range of 0.1 to 50%, preferably 1 to 30% for smoking agents or the like; and typically in a range of 0.05 to 20%, preferably 0.1 to 10% for aerosols or the like.

The formulation is sprayed after dilution in an appropriate concentration, or applied directly.

When present harmful organism control agent is used after dilution with a diluent, the concentration of the active ingredient is generally 0.1 to 5000 ppm. When the formulation is used per se, the application amount thereof per unit area is 0.1 to 5000 g per 1 ha in terms of the active ingredient compound; however, the application amount is not restricted thereto.

It goes without saying that the present harmful organism control agent is sufficiently effective when the present compound is used alone as an active ingredient. However, the present harmful organism control agent may be mixed or used in combination, as necessary, with other fertilizers and agricultural chemicals such as insecticide, miticide, nematicide, synergist, fungicide, antiviral agent, attractant, herbicide, plant growth-controlling agent, and the like. In this case, a more excellent effect can be exhibited.

Below are shown examples of known insecticides, miticides, nematicides, and synergist compounds, which may be mixed or used in combination. Insecticide active ingredients: acrinathrin, azadirachtin, azamethiphos, acynonapyr, azinphos-ethyl, azinphos-methyl, acequinocyl, acetamiprid, acetoprole, acephate, azocyclotin, abamectin, afidopyropen, afoxolaner, amidoflumet, amitraz, alanycarb, aldicarb, aldoxycarb, allethrin [including d-cis-trans-body, and d-trans-body], isazophos, isamidofos, isocarbophos, isoxathion, isofenphos-methyl, isoprocarb, epsilon-metofluthrin, epsilon-momfluorothrin, ivermectin, imicyafos, imidacloprid, imiprothrin, indoxacarb, esfenvalerate, ethiofencarb, ethion, ethiprole, ethylene dibromide, etoxazole, etofenprox, ethoprophos, etrimfos, emamectin, emamectin benzoate, endosulfan, empenthrin, oxazosulfyl, oxamyl, oxydemeton-methyl, oxydeprofos, omethoate, cadusafos, kappa-tefluthrin, kappa-bifenthrin, karanjin, cartap, carbaryl, carbosulfan, carbofuran, gamma-BHC, xylylcarb, quinalphos, kinoprene, chinomethionat, coumaphos, cryolite, clothianidin, clofentezine, chromafenozide, chlorantraniliprole, chlorethoxyfos, chlordane, chloropicrin, chlorpyrifos, chlorpyrifos-methyl, chlorfenapyr, chlorfenvinphos, chlorfluazuron, chlormephos, chloroprallethrin, cyazypyr, cyanophos, diafenthiuron, diamidafos, cyantraniliprole, dienochlor, cyenopyrafen, dioxabenzofos, diofenolan, cyclaniliprole, cycloxaprid, dicrotophos, dichlofenthion, cycloprothrin, dichlorvos, dicloromezotiaz, dicofol, dicyclanil, disulfoton, dinotefuran, dinobuton, cyhalodiamide, cyhalothrin [including gamma-body, and lambda-body], cyphenothrin [including (1R)-trans-body], cyfluthrin) [including beta-body], diflubenzuron, cyflumetofen, diflovidazin, cyhexatin, cypermethrin [including alpha-body, beta-body, theta-body, and zeta-body], dimethyl-2,2,2-trichloro-1-hydroxyethyl phosphate (DEP), dimethylvinphos, dimethoate, dimefluthrin, silafluofen, cyromazine, spinetoram, spinosad, spirodiclofen, spirotetramat, spiropidion, spiromesifen, sulcofuron-sodium, sulfluramid, sulfoxaflor, sulfotep, diazinon, thiacloprid, thiamethoxam, tioxazafen, thiodicarb, thiocyclam, thiosultap, thionazin, thiofanox, thiometon, tyclopyrazoflor, tetrachlorantraniliprole, tetrachlorvinphos, tetradifon, tetraniliprole, tetramethylfluthrin, tetramethrin, tebupirimfos, tebufenozide, tebufenpyrad, tefluthrin, teflubenzuron, demeton-S-methyl, temephos, deltamethrin, terbufos, tralomethrin, transfluthrin, triazamate, triazophos, trichlorfon, triflumuron, triflumezopyrim, trimethacarb, tolfenpyrad, naled, nicotine, nitenpyram, nemadectin, novaluron, noviflumuron, Verticillium lecanii, hydroprene, Bacillus sphaericus, Bacillus subtillis, Bacillus thuringiensis, insect toxin produced by Bacillus thuringiensis, Bacillus thuringiensis subsp. Aizawai, Bacillus thuringiensis subsp. Israelensis, Bacillus thuringiensis subsp. Kurstaki, Bacillus thuringiensis subsp. Tenebrionis, Bacillus popilliae, Pasteuriapenetrans spore, vamidothion, parathion, parathion-methyl, halfenprox, halofenozide, bioallethrin, bioallethrin S-cyclopentenyl, bioresmethrin, bis-(2-chloro-1-methylethyl)ether (DCIP), bistrifluron, hydramethylnon, bifenazate, bifenthrin, pyflubumide, piperonyl butoxide, pymetrozine, pyraclofos, pyrafluprole, pyridaphenthion, pyridaben, pyridalyl, pyrifluquinazon, pyriprole, pyriproxyfen, pirimicarb, pyrimidifen, pyriminostrobin, pirimiphos-methyl, pyrethrine, famphur, fipronil, fenazaquin, fenamiphos, fenitrothion, fenoxycarb, fenothiocarb, phenothrin [including (1R)-trans-body], fenobucarb, fenthion, phenthoate, fenvalerate, fenpyroximate, fenbutatin oxide, fenpropathrin, fonofos, sulfuryl fluoride, butocarboxim, butoxycarboxim, buprofezin, furathiocarb, prallethrin, fluacrypyrim, fluazaindolizine, fluazuron, fluensulfone, fluopyram, sodium fluoroacetate, fluxametamide, flucycloxuron, flucythrinate, flusulfamide, fluthrin, fluvalinate [including tau-body], flupyradifurone, flupyrazofos, flupyrimin, flufiprole, flufenerim, flufenoxystrobin, flufenoxuron, fluhexafon, flubendiamide, flumethrin, fluralaner, flurimfen, prothiofos, protrifenbute, flonicamid, propaphos, propargite, profenofos, broflanilide, profluthrin, propetamphos, propoxur, flometoquin, bromopropylate, hexythiazox, hexaflumuron, Pacilimyces tenuipes, Paecilomyces fumosoroceus, heptafluthrin, heptenophos, permethrin, benclothiaz, benzpyrimoxan, bensultap, benzoximate, bendiocarb, benfuracarb, Beauveria tenella, Beauveria bassiana, Beauveria brongniartii, phoxim, phosalone, fosthiazate, fosthietan, phosphamidon, phosmet, polynactins, formetanate, phorate, malathion, milbemectin, mecarbam, mesulfenfos, methomyl, metaldehyde, metaflumizone, methamidophos, metham, methiocarb, methidathion, methyl isothiocyanate, methyl bromide, methoxychlor, methoxyfenozide, methothrin, metofluthrin, methoprene, metolcarb, mevinphos, meperfluthrin, Monacrosporium phymatophagum, monocrotophos, momfluorothrin, litlure-A, litlure-B, aluminium phosphide, zinc phosphide, phosphine, lufenuron, rescalure, resmethrin, lepimectin, rotenone, nuclear polyhedrosis virus silkworm-embedded body, fenbutatin oxide, calcium cyanide, organotins, nicotine-sulfate, (Z)-11-tetradecenyl=acetate, (Z)-11-hexadecenal, (Z)— 11-hexadecenyl=acetate, (Z)-9,12-tetradecadienyl=acetate, (Z)-9-tetradecene-1-ol, (Z,E)-9,11-tetradecadienyl=acetate, (Z,E)-9,12-tetradecadienyl=acetate, 1,1,1-trichloro-2,2-bis(4-chlorophenyl)ethane (DDT), 1,3-dichloropropene(1,3-dichloropropene), 2,4-dichloro-5-{2-[4-(trifluoromethyl)phenyl]ethoxy}phenyl 2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472050-04-6), 2,4-dichloro-5-{2-[4-(trifluoromethyl)phenyl]ethoxy}phenyl 2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472052-11-1), 2,4-dimethyl-5-[6-(trifluoromethylthio)hexyloxy]phenyl-2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472050-34-2), 2-{2-fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenoxy}-5-(trifluoromethyl)pyridine (Chemical name, CAS registry number: 1448758-62-0), 3-chloro-2-{2-fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenoxy}-5-(trifluoromethyl)pyridine (Chemical name, CAS registry number: 1448761-28-1), 4,6-dinitro-o-cresol (DNOC), 4-fluoro-2-methyl-5-(5,5-dimethylhexyloxy]phenyl-2,2,2-trifluoroethyl sulfoxide (Chemical name, CAS registry number: 1472047-71-4), Bt protein (CrylAb, CrylAc, CrylFa, Cry2Ab, mCry3A, Cry3Ab, Cry3Bb, Cry34/35Ab1), CL900167 (code number), NA-85 (code number), NI-30 (code number), O,O-diethyl-O-[4-(dimethylsulfamoyl)phenyl]-phosphorothioate (DSP), O-ethyl-O-4-(nitrophenyl)phenylphosphonothioate (EPN), RU15525 (code number), XMC(XMC), Z-13-icosen-10-one, ZXI8901 (code number).

Next, examples of known bactericides or disease controller compounds that can be mixed or used in combination are shown below.

Bactericide active ingredients: azaconazole, acibenzolar-S-methyl, azoxystrobin, anilazine, amisulbrom, aminopyrifen, ametoctradin, aldimorph, isotianil, isopyrazam, isofetamid, isoflucypram, isoprothiolane, ipconazole, ipflufenoquin, ipfentrifluconazole, iprodione, iprovalicarb, iprobenfos, imazalil, iminoctadine-albesilate, iminoctadine-triacetate, imibenconazole, inpyrfluxam, imprimatin A, imprimatin B, edifenphos, etaconazole, ethaboxam, ethirimol, ethoxyquin, etridiazole, enestroburin, enoxastrobin, epoxiconazole, organic oils, oxadixyl, oxazinylazole, oxathiapiprolin, oxycarboxin, oxine-copper, oxytetracycline, oxpoconazole-fumarate, oxolinic acid, copper dioctanoate, octhilinone, ofurace, orysastrobin, o-phenylphenol, kasugamycin, captafol, carpropamid, carbendazim, carboxin, carvone, quinoxyfen, quinofumelin, chinomethionat, captan, quinconazole, quintozene, guazatine, cufraneb, coumethoxystrobin, coumoxystrobin, kresoxim-methyl, clozylacon, chlozolinate, chlorothalonil, chloroneb, cyazofamid, diethofencarb, diclocymet, dichlofluanid, dichlobentiazox, diclomezine, dicloran, dichlorophen, dithianon, diniconazole, diniconazole-M, zineb, dinocap, dipymetitrone, diphenylamine, difenoconazole, cyflufenamid, diflumetorim, cyproconazole, cyprodinil, simeconazole, dimethirimol, dimethyl disulfide, dimethomorph, cymoxanil, dimoxystrobin, Pseudomonas rhodesiae HAI-0804, ziram, silthiofam, streptomycin, spiroxamine, sedaxane, zoxamide, solatenol, dazomet, Talaromyces flavus, tiadinil, thiabendazole, thiram, thiophanate, thiophanate-methyl, thifluzamide, thiram, tecnazene, tecloftalam, tetraconazole, debacarb, tebuconazole, tebufloquin, terbinafine, dodine, dodemorph, triadimenol, triadimefon, triazoxide, trichlamide, triclopyricarb, Trichoderma atroviride, tricyclazole, triticonazole, tridemorph, triflumizole, trifloxystrobin, triforine, tolylfluanid, tolclofos-methyl, tolnifanide, tolprocarb, nabam, natamycin, naftifine, nitrapyrin, nitrothal-isopropyl, nuarimol, copper nonyl phenol sulphonate, Bacillus subtilis) (strain: QST 713, validamycin, valifenalate, picarbutrazox, bixafen, picoxystrobin, pydiflumetofen, bitertanol, binapacryl, hinokitiol, biphenyl, piperalin, hymexazol, pyraoxystrobin, pyraclostrobin, pyraziflumid, pyrazophos, pyrapropoyne, pyrametostrobin, pyriofenone, pyrisoxazole, pyridachlometyl, pyrifenox, pyributicarb, pyribencarb, pyrimethanil, pyroquilon, vinclozolin, ferbam, famoxadone, phenazine oxide, fenamidone, fenaminstrobin, fenarimol, fenoxanil, ferimzone, fenpiclonil, fenpicoxamid, fenpyrazamine, fenbuconazole, fenfuram, fenpropidin, fenpropimorph, fenhexamid, folpet, phthalide, bupirimate, fuberidazole, blasticidin-S, furametpyr, furalaxyl, furancarboxylic acid, fluazinam, fluindapyr, fluoxastrobin, fluopicolide, fluopimomide, fluopyram, fluoroimide, fluxapyroxad, fluquinconazole, furconazole, furconazole-cis, fludioxonil, flusilazole, flusulfamide, flutianil, flutolanil, flutriafol, flufenoxystrobin, flumetover, flumorph, proquinazid, prochloraz, procymidone, prothiocarb, prothioconazole, bronopol, propamocarb-hydrochloride, propiconazole, propineb, probenazole, bromuconazole, flometoquin, florylpicoxamid, hexaconazole, benalaxyl, benalaxyl-M, benodanil, benomyl, pefurazoate, penconazole, pencycuron, benzovindiflupyr, benthiazole, benthiavalicarb-isopropyl, penthiopyrad, penflufen, boscalid, fosetyl (alminium, calcium, sodium), polyoxin, polycarbamate, Bordeaux mixture, mancopper, mancozeb, mandipropamid, mandestrobin, maneb, myclobutanil, mineral oils, mildiomycin, methasulfocarb, metam, metalaxyl, metalaxyl-M, metiram, metyltetraprole, metconazole, metominostrobin, metrafenone, mepanipyrim, mefentrifluconazole, meptyldinocap, mepronil, iodocarb, laminarin, Rhizobium vitis, phosphorous acid and salts, copper oxychloride, silver, cuprous oxide, copper hydroxide, potassium bicarbonate, sodium bicarbonate, sulfur, oxyquinoline sulfate, copper sulfate, (3,4-dichloroisothiazole-5-yl)methyl 4-(tert-butyl)benzoic ester (Chemical name, CAS registry number: 1231214-23-5), BAF-045 (code number), BAG-010 (code number), UK-2A (code number), dodecylbenzenesulfonic acid bisethylenediamine copper [II] salt (DBEDC), MIF-1002 (code number), NF-180 (code number), triphenyltin acetate (TPTA), triphenyltin chloride (TPTC), triphenyltin hydroxide (TPTH), avirulent Erwinia carotovora.

Next, examples of known herbicides or plant growth regulator compounds that can be mixed or used in combination are shown below.

Herbicide active ingredients: ioxynil, aclonifen, acrolein, azafenidin, acifluorfen (including a salt with sodium or the like), azimsulfuron, asulam, acetochlor, atrazine, anilofos, amicarbazone, amidosulfuron, amitrole, aminocyclopyrachlor, aminopyralid, amiprofos-methyl, ametryn, alachlor, alloxydim, ancymidol, isouron, isoxachlortole, isoxaflutole, isoxaben, isodecylalkoholethoxylat, isoproturon, ipfencarbazone, imazaquin, imazapic (including a salt with amine or the like), imazapyr (including a salt of isopropylamine or the like), imazamethabenz-methyl, imazamox, imazethapyr, imazosulfuron, indaziflam, indanofan, eglinazine-ethyl, esprocarb, ethametsulfuron-methyl, ethalfluralin, ethidimuron, ethoxysulfuron, ethoxyfen-ethyl, ethofumesate, etobenzanid, endothal-disodium, oxadiazon, oxadiargyl, oxaziclomefone, oxasulfuron, oxyfluorfen, oryzalin, orthosulfamuron, orbencarb, oleic acid, cafenstrole, carfentrazone-ethyl, karbutilate, carbetamide, quizalofop, quizalofop-ethyl, quizalofop-P-ethyl, quizalofop-P-tefuryl, quinoclamine, quinclorac, quinmerac, cumyluron, clacyfos, glyphosate (including a salt of sodium, potassium, amine, propylamine, isopropylamine, dimethylamine, trimesium, or the like), glufosinate (including a salt of amine, sodium, or the like), glufosinate-P, glufosinate-P-sodium, clethodim, clodinafop-propargyl, clopyralid, clomazone, chlomethoxyfen, clomeprop, cloransulam-methyl, chloramben, chloridazon, chlorimuron-ethyl, chlorsulfuron, chlorthal-dimethyl, chlorthiamid, chlorphthalim, chlorflurenol-methyl, chlorpropham, chlorbromuron, chloroxuron, chlorotoluron, ketospiradox (including a salt of sodium, calcium, ammonia, or the like), saflufenacil, sarmentine, cyanazine, cyanamide, diuron, diethatyl-ethyl, dicamba (including a salt of amine, diethylamine, isopropylamine, diglycolamine, sodium, lithium, or the like), cycloate, cycloxydim, diclosulam, cyclosulfamuron, cyclopyranil, cyclopyrimorate, dichlobenil, diclofop-P-methyl, diclofop-methyl, dichlorprop, dichlorprop-P, diquat, dithiopyr, siduron, dinitramine, cinidon-ethyl, cinosulfuron, dinoseb, dinoterb, cyhalofop-butyl, diphenamid, difenzoquat, diflufenican, diflufenzopyr, simazine, dimethachlor, dimethametryn, dimethenamid, dimethenamid-P, simetryn, dimepiperate, dimefuron, cinmethylin, swep, sulcotrione, sulfentrazone, sulfosate, sulfosulfuron, sulfometuron-methyl, sethoxydim, terbacil, daimuron, thaxtomin A, dalapon, thiazopyr, tiafenacil, thiencarbazone (including sodium salt, methyl ester, or the like), tiocarbazil, thiobencarb, thidiazimin, thidiazuron, thifensulfuron-methyl, desmedipham, desmetryne, thenylchlor, tebutam, tebuthiuron, tepraloxydim, tefuryltrione, terbuthylazine, terbutryn, terbumeton, tembotrione, topramezone, tralkoxydim, triaziflam, triasulfuron, triafamone, tri-allate, trietazine, triclopyr, triclopyr-butotyl, tritosulfuron, trifludimoxazin, triflusulfuron-methyl, trifluralin, trifloxysulfuron-sodium, tribenuron-methyl, tolpyralate, naptalam (including a salt with sodium or the like), naproanilide, napropamide, napropamide-M, nicosulfuron, neburon, norflurazon, vemolate, paraquat dichloride, halauxifen-benzyl, halauxifen-methyl, haloxyfop, haloxyfop-P, haloxyfop-etotyl, halosafen, halosulfuron-methyl, picloram, picolinafen, bicyclopyrone, bispyribac-sodium, pinoxaden, bifenox, piperophos, pyraclonil, pyrasulfotole, pyrazoxyfen, pyrazosulfuron-ethyl, pyrazolynate, bilanafos, pyraflufen-ethyl, pyridafol, pyrithiobac-sodium, pyridate, pyriftalid, pyributicarb, pyribenzoxim, pyrimisulfan, pyriminobac-methyl, pyroxasulfone, pyroxsulam, phenisopham, fenuron, fenoxasulfone, fenoxaprop (including methyl, ethyl, isopropylester), fenoxaprop-P (including methyl, ethyl, isopropyl ester), fenquinotrione, fenthiaprop-ethyl, fentrazamide, phenmedipham, foramsulfuron, butachlor, butafenacil, butamifos, butylate, butenachlor, butralin, butroxydim, flazasulfuron, flamprop (including methyl, ethyl, isopropyl ester), flamprop-M (including methyl, ethyl, isopropyl ester), primisulfuron-methyl, fluazifop-butyl, fluazifop-P-butyl, fluazolate, fluometuron, fluoroglycofen-ethyl, flucarbazone-sodium, fluchloralin, flucetosulfuron, fluthiacet-methyl, flupyrsulfuron-methyl (including a salt of sodium, calcium, ammonia, or the like), flufenacet, flufenpyr-ethyl, flupropanate, flupoxame, flumioxazin, flumiclorac-pentyl, flumetsulam, fluridone, flurtamone, fluroxypyr (including an ester such as butomethyl or meptyl, a salt of sodium, calcium, ammonia, or the like), flurochloridone, pretilachlor, procarbazone-sodium, prodiamine, prosulfuron, prosulfocarb, propaquizafop, propachlor, propazine, propanil, propyzamide, propisochlor, propyrisulfuron, propham, profluazol, prohexadione-calcium, propoxycarbazone, propoxycarbazone-sodium, profoxydim, bromacil, brompyrazon, prometryn, prometon, bromoxynil (including an ester of butyric acid, octanoic acid, heptanoic acid, or the like), bromofenoxim, bromobutide, florasulam, florpyrauxifen, florpyrauxifen-benzyl, hexazinone, pethoxamid, benazolin, penoxsulam, heptamaloxyloglucan, beflubutamid, pebulate, pelargonic acid, bencarbazone, pendimethalin, benzfendizone, bensulide, bensulfuron-methyl, benzobicyclon, benzofenap, bentazone, pentanochlor, pentoxazone, benfluralin, benfuresate, fosamine, fomesafen, foramsulfuron, forchlorfenuron, mecoprop (including a salt of sodium, potassium, isopropylamine, triethanolamine, dimethylamine, or the like), mecoprop-P-potassium, mesosulfuron (including an ester of methyl or the like), mesotrione, metazachlor, metazosulfuron, methabenzthiazuron, metamitron, metamifop, metam, disodium methanearsonate (DSMA), methiozolin, methyldymuron, metoxuron, metosulam, metsulfuron-methyl, metobromuron, metobenzuron, metolachlor, metribuzin, mepiquat chloride, mefenacet, monosulfuron (including methyl, ethyl, isopropylester), monolinuron, molinate, iodosulfuron, iodosulfulon-methyl-sodium, iofensulfuron, iofensulfuron-sodium, lactofen, lancotrione, linuron, rimsulfuron, lenacil, 2,2,2-trichloroacetic acid (TCA) (including a salt of sodium, calcium, ammonia, or the like), 2,3,6-trichlorobenzoic acid (2,3,6-TBA), 2,4,5-trichlorophenoxyacetic acid (2,4,5-T), 2,4-dichlorophenoxyacetic acid (2,4-D) (including a salt of amine, diethylamine, triethanolamine, isopropylamine, sodium, lithium, or the like), 2-amino-3-chloro-1,4-naphthoquinone (ACN), 2-methyl-4-chlorophenoxyacetic acid (MCPA) (including a sodium salt, ethyl ester, or the like), 2-methyl-4-chlorophenoxyacetic acid (MCPB) (including a sodium salt, ethyl ester, or the like), 4-(2,4-dichlorophenoxy)butyric acid (2,4-DB), 4,6-dinitro-O-cresol (DNOC) (including a salt of amine, sodium, or the like), AE-F-150944 (code number), F9600 (code number), IR-6396 (code number), MCPA-thioethyl, SYP-298 (code number), SYP-300 (code number), S-ethyldipropylthiocarbamate (EPTC), S-metolachlor, S-9750 (code number), MSMA, HW-02 (code number).

Plant growth regulators: 1-naphthylacetamide, 1-methylcyclopropene, 2,6-diisopropylnaphthalene, 4-oxo-4-(2-phenylethyl)aminobutyric acid (Chemical name, CAS registry number: 1083-55-2), 4-chlorophenoxyacetic acid (4-CPA), n-decanol, aviglycine, ancymidol, abscisic acid, inabenfide, indole acetic acid, indole butyric acid, uniconazole, uniconazole-P, Ecolyst, ethychlozate, ethephon, epocholeone, oxine-sulfate, carvone, calcium formate, cloxyfonac, cloxyfonac-potassium, cloprop, chlormequat, choline, cytokinins, cyclanilide, dikegulac, gibberellin acid, dimethipin, sintofen, daminozide, thidiazuron, triacontanol, trinexapac-ethyl, paclobutrazol, paraffin, flumetralin, flurprimidol, flurenol, prohydrojasmon, prohexadione-calcium, heptamaloxyloglucan, benzylaminopurine, forchlorfenuron, maleic hydrazide, mepiquat chloride, mefluidide, calcium peroxide.

Next, examples of known phytotoxicity alleviating compounds that can be mixed or used in combination are shown below.

Isoxadifen, isoxadifen-ethyl, oxabetrinil, cloquintcet-mexyl, dietholate, cyometrinil, dichlormid, dicyclonone, cyprosulfamide, 1,8-Naphthalic Anhydride, fenchlorazole-O-ethyl, fenclorim, furilazole, fluxofenim, flurazole, benoxacor, mephenate, mefenpyr, mefenpyr-ethyl, mefenpyr-diethyl, lower alkyl-substituted benzoic acid, 2,2-dichloro-N-(1,3-dioxane-2-ylmethyl)-N-(2-propenyl)acetamide (PPG-1292), 2-dichloromethyl-2-methyl-1,3-dioxane (MG-191), 3-dichloroacetyl-2,2,5-trimethyl-1,3-oxazolidine (R-29148), 4-dichloroacetyl-1-oxa-4-azaspiro[4.5]decane (AD-67), MON4660 (code number), metcamifen, N1,N2-diallyl-N2-dichloroacetyl glycineamide (DKA-24), TI-35 (code number).

The present harmful organism control agent configured as described above exhibits excellent controlling effect on Orthoptera pests, Thysanoptera pests, Hemiptera pests, Coleoptera pests, Diptera pests, Lepidoptera pests, Hymenoptera pests, Collembola pests, Thysanura pests, Blattodea pests, Isoptera pests, Psocoptera pests, Mallophage pests, Anoplura pests, plant parasitic Acari, plant parasitic nematoda, plant parasitic mollusks, and other harmful organisms such as harmful animals, uncomfortable animals, sanitary insects, and parasites. As such harmful organisms, the following organism species can be exemplified.

Examples of the Orthopteran pests include Ruspolia lineosa or the like of Tettigoniidae, Teleogryllus emma, Truljalia hibinonis, or the like of Gryllidae, Gryllotalpa orientalis or the like of Gryllotalpidae, Oxya hyla intricate, Locusta migratoria, Melanoplus sanguinipes, Melanoplus differentialis, Melanoplus femurrubrum, or the like of Acrididae, Atractomorpha lata of Pyrgomorphidae, Euscyrtus japonicus of Eneopteridae, and Xya japonicus or the like of Tridactylidae.

Examples of the Thysanoptera pests include Frankliniella intonsa, Frankliniella occidentalis, Scirtothrips dorsalis, Thrips palmi, Thrips tabaci, Thrips setosus, Heliothrips haemorrhoidalis, Stenchaetothrips biformis, or the like of Thripidae, and Ponticulothrips diospyrosi, Liothrips wasabiae, Haplothrips aculeatus, or the like of Phlaeothripidaes.

Examples of the Hemipteran pests include Mogannia minuta or the like of Cicadidae, Aphrophora intermedia or the like of Aphrophoridae, Machaerotypus sibiricus or the like of Membracidae, Arboridia apicalis, Empoasca onukii, Nephotettix cincticeps, Nephotettix malayanus, Nephotettix virescens, Nephotettix nigropictus, Recilia dorsalis, Okura Leafhopper (Amrasca biguttula), Mango Leafhopper (Idioscopus nitidulus, Idioscopus clypealis, Amritodus atkinsoni), Empoasca fabae, or the like of Cicadellidae, Pentastiridius apicalis or the like of Cixiidae, Laodelphax striatellus, Nilaparvata lugens, Sogatella furcifera, or the like of Delphacidae, Nisia nervosa or the like of Meenoplidae, Kamendaka saccharivora or the like of Derbidae, Achilus flammeus or the like of Cixidia, Orosanga japonicus or the like of Ricaniidae, Mimophantia maritima or the like of Flatidae, Cacopsylla pyrisuga, Diaphorina citri, or the like of Psyllidae, Calophya mangiferae or the like of Calophyidae, Daktulosphaira vitifoliae or the like of Phylloxeridae, Adelges laricis, Adelges tsugae, or the like of Adelgidae, Acyrthosiphon pisum, Aphis gossypii, Aphis spiraecola, Lipaphis erysimi, Brevicoryne brassicae, Myzuspersicae, Schizaphis graminum, Rhopalosiphum padi, Toxoptera aurautii, Aulacorthum solani, Macrosiphum euphorbiae, Nasonovia ribisnigri, Sitobion avenae, Aphis glycines, or the like of Aphydidae, Aleurocanthus camelliae, Aleurocanthus spiniferus, Bemisia tabaci, Bemisia argentifolii, Trialeurodes vaporariorum, or the like of Aleyrodidae, Drosicha corpulenta, Icerya purchasi, or the like of Margarodidae, Dysmicoccus brevipes, Planococcus citri, Pseudococcus comstocki, or the like of Pseudococcidae, Ceroplastes ceriferus, Ceroplastes rubens, or the like of Coccidae, Aclerda takahashii or the like of Aclerdidae, Aonidiella aurantii, Diaspidiotus pemiciosus, Pseudaulacaspis pentagoa, Unaspis yanonensis, or the like of Diaspididae, Lygus lineolaris, Trigonotylus caelestialium, Apolygus lucorum, Nesidiocoris tenuis, Halticus bractatus, or the like of Miridae, Stephanitis pyrioides, Stephanitis nashi, or the like of Tingidae, Eurydema rugosum, Eysarcoris lewisi, Eysarcoris aeneus, Lagynotomus elongatus, Nezara viridula, Plautia crossota, Nezara antennata, Eushistus heros, or the like of Pentatomidae, Megacopta cribraria or the like of Plataspidae, Urochela luteovoria or the like of Urostylididae, Cavelerius saccharivorus or the like of Lygaeidae, Malcus japonicus or the like of Malcidae, Dysdercus cingulatus or the like of Pyrrhocoridae, Leptocorisa acuta, Leptocorisa chinensis, or the like of Alydidae, Anacanthocoris striicomis or the like of Coreidae, Rhopalus maculatus or the like of Rhopalidae, and Cimex lectularis or the like of Cimicidae.

Examples of the Coleoptera pests include Anomara cuprea, Anomara rufocuprea, Popilliaj aponica, Oxycetonia jucunda, Anomala geniculata, Oryctes rhinoceros, Heptophylla picea, or the like of Scarabaeidae, Agriotes ogurae, Agriotes lineatus, Agriotes obscurus, Melanotus okinawensis, Melanotus fortnumi, or the like of Elateridae, Anthrenus verbasci or the like of Dermestidae, Heterobostrychus hamatipennis or the like of Bostrychidae, Stegobium paniceum or the like of Anobiidae, Pitinus clavipes or the like of Ptinidae, Tenebroides mauritanicus or the like of Trogossitidae, Necrobia rufipes of Cleridae, Carpophilus hemipterus, Meligethes aeneus, or the like of Nitidulidae, Ahasverus advena or the like of Silvanidae, Cryptolestes ferrugineus or the like of Laemophloeidae, Epilachna varivestis, Henosepilachna vigintioctopunctata or the like of Coccinellidae, Tenebrio molitor, Tribolium castaneum, or the like of Tenebrionidae, Epicauta gorhami or the like of Meloidae, Anoplophora glabripennis, Xylotrechus pyrrhoderus, Monochamus alternatus, Dectes texanus, or the like of Cerambycidae, Callosobruchus chinensis or the like of Bruchidae, Leptinotarsa decemlineata, Diabrotica virgifera virgifera, Diabrotica barberi, Diabrotica undecimpunctata howardi, Aulacophora femoralis, Phaedon brassicae, Cassida nebulosa, Oulema oryzae, Epilachna varivestis, Phyllotreta striolata, Demotina fasciculata, Psylliodes chrysocephala, Cerotoma trifurcate, Colaspis brunnea, Colaspis crinnicornis, Odontota homi, Chaetocnema pulicaria, or the like of Chrysomelidae, Cylas formicarius or the like of Brentidae, Hypera postica, Listroderes costirostris, Euscepes postfasciatus, Curculio sikkimensis, or the like of Curculionidae, Echinocnemus bipunctatus, Lissorhoptrus oryzophilus, Oryzophagus oryzae, or the like of Erirhinidae, Sitophilus zeamais, Sphenophrus venatus, or the like of Dryophthoridae, Tomicus piniperda or the like of Scolytidae, Crossotarsus niponicus or the like of Platypodidae, and Lyctus brunneus or the like of Lyctidae.

Examples of the Diptera include Tipula aino or the like of Tipulidae, Plecia nearctica or the like of Bibionidae, Exechia shiitakevora or the like of Mycetophidae, Pnyxiascabiei, Bradysia agrestis, or the like of Sciaridae, Asphondylia yushimai, Mayetiola destructor, Dasineura oxycoccana, or the like of Cecidomyiidae, Aedes aegypti, Culex pipiens pallens, or the like of Culicidae, Simulium takahashii or the like of Simuliidae, Chironomus oryzae or the like of Chironomidae, Chrysops suavis, Tabanus trigonus, or the like of Tabanidae, Eumerus strigatus or the like of Syrphidae, Bactrocera dorsalis, Euphranta japonica, Ceratitis capitata, or the like of Tephritidae, Liriomyza trifolii, Liriomyza sativae, Agromyza oryzae, Liriomyza bryoniae, Chromatomyia horticola, Liriomyza chinensis, Liriomyza trifolii, or the like of Agromyzidae, Meromyza nigriventris or the like of Chloropidae, Drosophila suzukii, Drosophila melanogaster, or the like of Drosophilidae, Hydrellia griseola or the like of Ephydridae, Hippobosca equina or the like of Hippoboscidae, Parallelpmma sasakawae or the like of Scatophagidae, Delia antiqua, Delia platura, or the like of Anthomyiidae, Fannia canicularis or the like of Fanniidae, Musca domestica, Stomoxys calcitrans or the like of Muscidae, Sarcophaga peregrina or the like of Sarcophagidae, Gasterophilus intestinalis or the like of Gasterophilidae, Hypoderma lineatum or the like of Hypodermatidae, and Oestrus ovis or the like of Oestridae.

Examples of the Lepidoptera include Endoclita excrescens or the like of Hepialidae, Antispila ampelopsia or the like of Heliozelidae, Zeuzera leuconotum, Cossus insularis, or the like of Cossidae, Archips fuscocupreanus, Adoxophyes orana fasciata, Grapholita molesta, Homona magnanima, Leguminivora glycinivorella, Cydia pomonella, Lobesia botrana, or the like of Tortricidae, Eupoecilia ambiguella or the like of Cochylidae, Bambalina sp., Eumeta minuscula, or the like of Psychidae, Nemapogon granella, Tinea translucens, or the like of Tineidae, Bucculatrix pyrivorella or the like of Bucculatricidae, Lyonetia clerkella, Lyonetiaprunifoliella malinella, or the like of Lyonetiidae, Caloptilia theivora, Phyllonorycter ringoniella, or the like of Gracilariidae, Phyllocnistis citrella or the like of Phyllocnistidae, Acrolepiopsis sapporensis or the like of Acrolepiidae, Plutella xylostella of Plutellidae, Yponomeuta orientalis, or the like of Yponomeutidae, Argyresthia conjugella or the like of Argyresthidae, Nokona regalis, Synanthedin hector or the like of Sesidae, Phthorimaea operculella, Sitotroga cerealella, Pectinophora gossypiella, Tuta absoluta, or the like of Gelechiidae, Carposina sasakii or the like of Carposinidae, Illiberis pruni or the like of Zygaenidae, Monema flavescens or the like of Limacodidae, Ancylolomia japonica, Chilo suppressalis, Cnaphalocrocis medinalis, Ostrinia fumacalis, Hellulla undalis, Conogethes punctiferlis, Diaphania indica, Parapediasia teterrella, Ostrinia nubilalis, or the like of Crambidae, Diatraea saccharalis, Cadra cautella, Galleria mellonella, or the like of Pyralidae, Nippoptilia vitis or the like of Pterophoridae, Papilio xuthus or the like of Papilionidae, Pieris rapae or the like of Pieridae, Parnara guttata or the like of Hesperiidae, Ascotis selenaria or the like of Geometridae, Dendrolimus spectabilis, Malacosoma neustrium testaceum, or the like of Lasiocampidae, Agrius convolvuli or the like of Sphingidae, Ama pseudoconspersa, Orygia recens approximans, Lymantria dispar, or the like of Lymantriidae, Hyphantria cunea or the like of Arctiidae, and Agrotis ipsilon, Agrotis segetum, Autographa nigrisigna, Helicoverpa armigera, Helicoverpa zea, Heliothis virescens, Spodoptera exigua, Spodoptera litura, Chrysodeix includens, Spodoptera frugiperda, Nephelodes minians, or the like of Noctuidae.

Examples of the Hymenoptera pests include Arge pagana or the like of Argidae, Apethymus kuri, Athalia rosae ruficomis, or the like of Tenthredinidae, Dryocosmus kuriphilus, or the like of Cynipidae, Vespa simillima xanthoptera or the like of Vespidae, Solenopsis invicta, Linepithema humile, or the like of Formicidae, and Megachile nipponica or the like of Megachilidae.

Examples of the Collembola pests include Bourletiella hortensis or the like of Sminthuridae.

Examples of the Thysanura pests include Lepisma saccharina, Ctenolepisma villosa, or the like of Lepismatidae.

Examples of the Blattodea pests include Periplaneta americana of Blattidae, and Blattella germanica or the like of Blattellidae.

Examples of the Isoptera pests include Incisitermes minor or the like of Kalotermitidae, Coptotermes formosanus or the like of Rhinotermitidae, and Odontotermes formosanus or the like of Termitidae.

Examples of the Psocoptera pests include Trogium pulsatorium or the like of Trogiidae, and Liposcelis corrodens or the like of Liposcelididae.

Examples of the Dermaptera pests include Labodura riparia or the like of Labiduridae.

Examples of the Mallophaga pests include Lipeurus caponis or the like of Menoponidae, and Damalinia bovis or the like of Trichodectidae.

Examples of the Anoplura pests include Haematopinus suis or the like of Haematopinidae, Pediculus humanus or the like of Pediculine, Linognathus setosus or the like of Linognathidae, and Pthirus pubis or the like of Pthiridae

Examples of the Acari pests include Penthaleus major or the like of Eupodidae, Phytonemus pallidus, Polyphagotarsonemus latus, or the like of Tarsonemidae, one species of Siteroptes sp. or the like of Pyemotidae, Brevipalpus lewisi or the like of Tenuipalpidae, Tuckerella pavoniformis or the like of Tuckerellidae, Eotetrany chusboreus, Panonychus citri, Panonychus ulmi, Tetranychus urticae, Tetranychus kanzawai, or the like of Tetranychidae, Trisetacus pini or the like of Nalepellidae, Aculops pelekassi, Epitrimerus pyri, Phyllocoptruta oleivora, Aculops lycopersici, or the like of Eriophyidae, Diptacus crenatae or the like of Diptilomiopida, Aleuroglyphus ovatus, Tyrophagus putrescentiae, or Rhizoglyphus robini of Acaridae, Omithonyssus sylvialum or the like of Macronyssidae, Varroaj acobsoni or the like of Varroidae, Dermanyssus gallinae or the like of Dermanyssidae, Omithonyssus sylvialum or the like of Macronyssidae, Boophilus microplus, Rhipicephalus sanguineus, Haemaphysalis longicornis, or the like of Ixodidae, and Sarcoptes scabiei or the like of Sarcoptidae.

Examples of the plant parasitic nematoda, include Xiphinema index or the like of Longidoridae, Paratrichodorus minor or the like of Trichodoridae, one species of Rhabditidae (Rhabditella sp.) or the like, one species of Tylenchidae (Aglenchus sp.) or the like, one species of Tylodoridae (Cephalenchus sp.) or the like, Nothotylenchus acris, Ditylenchus destructor, or the like of Anguinidae, Rotylenchulus reniformis, Helicotylenchus dihystera, or the like of Hoplolaimidae, Paratylenchus curvitatus or the like of Paratylenchidae, Meloidogyne incognita, Meloidogyne hapla, or the like of Meloidogynidae, Globodera rostochiensis, Globodera pallida, Heterodera glycines, or the like of Heteroderidae, Tylenchorhynchus claytoni or the like of Telotylenchidae, one species of Psilenchidae (Psilenchus sp.) or the like, one species of Criconematidae (Criconemoides sp.) or the like, Tylenchulus semipenetrans or the like of Tylenchulidae, Sphaeronema camelliae or the like of Sphaeronematidae, Sphaeronema camelliae, Radopholus citrophilus, Radopholus similis, Nacobbus aberrans, Pratylenchus penetrans, Pratylenchus coffeae, or the like of Pratylenchidae, Iotonchium ungulatum or the like of Iotonchiidae, Aphelenchus avenae or the like of Aphelenchidae, Aphelenchoides besseyi, Aphelenchoides fragariae, or the like of Aphelenchoididae, and Bursaphelenchus xylophilus or the like of Palasitaphelenchidae.

Examples of the plant parasitic mollusks include Pomacea canaliculata or the like of Pilidae, Leavicaulis alte or the like of Veronicellidae, Achatina fulica or the like of Achatinidae, Meghimatium bilineatum or the like of Philomycidae, Succinealauta or the like of Succineidae, Discus pauper or the like of Didcidae, Zonitoides yessoensis or the like of Zonitidae, Limax flavus, Lehmannia valentiana, Deroceras reticulatum, or the like of Limacidae, Parakaliella harimensis or the like of Helicarionidae, and Acusta despecta sieboldiana, Bradybaena similaris, or the like of Bradybaenidae.

Examples of other harmful organisms such as harmful animals, uncomfortable animals, sanitary insects, livestock insects, and parasites include Procambarus clarkii or the like of Decapoda Astacidae, Armadillidium vulgare or the like of Isopoda Porcellionidae, Armadillidium vulgare or the like of Armadillidiidae, Chilopoda pests such as Scutigeromorpha Sutigeridae, Scolopendra subspinipes, or the like, Diplopoda pests such as Oxidus gracilis, Theridiidae hasseltii or the like of Araneae Latrodectus hasseltii, Chiracanthium japonicum, or the like of Clubionidae, Androctonus crassicauda or the like of Scorpiones, roundworm endoparasites such as Ascaris lumbricoides or the like, Syphacia sp. or the like, and Wuchereria bancrofti or the like, and flatworm endoparasites such as Distomum sp., Paragonimus westermanii, Metagonimus yokokawai, Schistosoma japonicum, Taenia solium, Taeniarhynchus saginatus, Echinococcus sp., or Diphyllobothrium latum.

The present harmful organism control agent exhibits a controlling effect also on the harmful organisms and the like exemplified above that have acquired the resistance to existing harmful organism control agents. Furthermore, the present harmful organism control agent can be applied to plants that have acquired characteristics such as pest tolerance, disease tolerance, herbicide tolerance, or the like by gene recombination, artificial mating, or the like.

Next, the production methods, formulation methods and applications of the present compound will be described in detail by way of Examples. However, the present invention is in no way restricted by these Examples. The melting point which is a physical property value of the present compound was determined by a MP-500V micro melting point measuring apparatus available from Yanaco. The refractive index was determined by using an Abbe refractometer available from ATAGO CO., LTD. ¹H NMR spectrum was determined by using JNM-LA400 (400 MHz), JNM-LA300 (300 MHz) or JNM-ECS300 (300 MHz) available from JEOL Ltd. and tetramethylsilane (TMS) as the internal standard. A high resolution mass spectrum (HRMS) was measured by using Q Exactive Focus Hybrid Quadrupole-Orbitrap LC-MS/MS System (ESI, positive mode) available from Thermo Fisher Scientific.

Methods for producing production intermediates of the present compound are also described.

EXAMPLES Example 1 Production of 4-(2,2,3,3,3-pentafluoropropoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0044) 1) Ethyl 4-(2,2,3,3,3-pentafluoropropoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: B-0298)

Ethyl 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (2.5 g, 10.7 mmoL) synthesized by the method described in Reference examples 1 and 2 of WO 2016/027790 A, 2,2,3,3,3-pentafluoropropyl nonafluorobutanesulfonate (4.7 g, 10.9 mmoL) and potassium carbonate, anhydrous (1.6 g, 11.6 mmoL) were sequentially added at room temperature to dimethyl sulfoxide (50 mL) and further stirred for 3 hours. The reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography, to give ethyl 4-(2,2,3,3,3-pentafluoropropoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (3.3 g, yield: 84%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 1.45 (3H, t), 4.47 (2H, q), 4.54 (2H, t), 7.45 (1H, dd), 7.81 (1H, s), 8.11 (1H, d), 8.63 (1H, d), 8.96 (1H, d)

2) 4-(2,2,3,3,3-pentafluoropropoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0044)

Ethyl 4-(2,2,3,3,3-pentafluoropropoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (1.2 g, 3.3 mmoL) was dissolved in methanol (100 mL), and aqueous ammonia (content: 28%, 50 mL) was further added and stirred at room temperature for 12 hours. The solvent of the reaction solution was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give 4-(2,2,3,3,3-pentafluoropropoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.8 g, yield: 72%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 4.68 (2H, t), 5.95 (1H, br), 6.81 (1H, br), 7.45 (1H, dd), 7.91 (1H, s), 8.06 (1H, d), 8.63 (1H, d), 8.97 (1H, d)

Example 2 Production of 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0240) 1) Ethyl 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: B-0494)

In a solution of ethyl 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (7.5 g, 32.2 mmoL) in N,N-dimethylformamide (150 mL), sodium hydride (content 60%, 1.5 g, 37.5 mmoL) was added little by little at room temperature, and stirred for about 30 minutes. To this reaction solution, benzyl bromide (5.5 g, 32.2 mmoL) was added at room temperature, and allowed to react for 1 hour. The reaction solution was poured into saturated brine, and extracted with ethyl acetate. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The obtained solid was washed with hexane, to give ethyl 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (8.1 g, yield: 78%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 1.44 (3H, t), 4.47 (2H, q), 5.15 (2H, s), 7.32-7.48 (6H, m), 7.56 (1H, s), 8.09 (1H, d), 8.58 (1H, d), 8.89 (1H, d)

2) 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0240)

Ethyl 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (7.5 g, 23.2 mmoL) was dissolved in ethanol (200 mL), and potassium hydroxide (10.0 g, 178.2 mmoL) and water (20 mL) were added at room temperature, and stirred for 1 hour. The solvent of the reaction solution was distilled off under reduced pressure, and 6 N hydrochloric acid was added to the residue, and the precipitated solid was collected by filtration, and dried to give crude 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid. The obtained 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid was dissolved in dichloromethane (200 mL), and oxalyl chloride (10 g, 78.8 mmoL) and N,N-dimethylformamide (catalytic amount) were added, and allowed to react at room temperature for 13 hours. The solution was distilled off under reduced pressure, and the residue was dissolved in ethyl acetate (50 mL). The solution was added to a mixed solution of ethyl acetate (200 mL) and aqueous ammonia (content: 28%, 50 mL) at 0° C., and then stirred at room temperature for 1 hour. The solvent in the reaction solution was distilled off under reduced pressure, and the residue was extracted with ethyl acetate and dried over anhydrous magnesium sulfate, and then the solvent was distilled off. The obtained solid was washed with hexane, to give 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (5.5 g, yield: 81%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 6.04 (1H, br), 6.95 (1H, br), 7.36-7.47 (6H, m), 7.63 (1H, s), 8.11 (1H, d), 8.57 (1H, d), 8.90 (1H, d)

Example 3 Production of 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (Present Compound Number: A-0071) 1) 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0001)

In ethanol (100 mL), 4-benzyloxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (1.5 g, 5.1 mmoL) was dissolved, and palladium activated carbon (content: 10%, 0.5 g) was added, and hydrogen (120 mL) was introduced over 2 hours. The reaction solution was filtered, and the solvent was distilled off under reduced pressure. The residue was washed with hexane to give 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.55 g, yield: 53%).

¹H-NMR data (400 MHz, DMSO-d6/TMS δ (ppm)): 7.56 (1H, dd), 7.62 (1H, br), 7.69 (1H, br), 8.21 (1H, s), 8.24 (1H, d), 8.54 (1H, d), 9.13 (1H, d), 9.35 (1H, br)

2) 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (Present Compound Number: A-0071)

In a mixed solvent of N,N-dimethylformamide (100 mL) and triethylamine (20 mL), 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.9 g, 4.4 mmoL) was added. In the reaction solution, (trifluoromethyl)(trifluorovinyl) ether (2 g, 12.0 mmoL) was introduced at 50° C. over about 30 minutes, and further stirred for 30 minutes. After end of the reaction, the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography to give 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (0.8 g, yield: 49%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 5.77 (1H, br), 6.17 (1H, d), 6.72 (1H, br), 7.48 (1H, dd), 8.05 (1H, s), 8.06 (1H, d), 8.67 (1H, d), 9.01 (1H, d)

Example 4 Production of 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0017) 1) Ethyl 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (Present Compound Number: B-0271)

Ethyl 4-hydroxy-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (1.0 g, 4.3 mmoL), 3,3-dimethylbutanol (0.53 g, 5.2 mmoL) and triphenylphosphine (1.4 g, 5.2 mmoL) were dissolved in THF (50 mL), and diisopropyl azodicarboxylate (1.1 g, 5.2 mmoL) was added under cooling on ice, and stirred overnight at room temperature. After end of the reaction, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give ethyl 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (1.27 g, yield: 93%).

¹H-NMR data (300 MHz, CDCl₃/TMS δ (ppm)): 1.02 (9H, s), 1.42 (3H, t), 1.82 (2H, t), 4.07 (2H, t), 4.44 (2H, q), 7.43 (1H, dd), 7.62 (1H, s), 8.15 (1H, d), 8.59 (1H, d), 8.96 (1H, d)

2) 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (Present Compound Number: B-0017)

Ethyl 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylate (1.1 g, 3.4 mmoL) was dissolved in ethanol (30 mL), and a mixed solution of sodium hydroxide (0.33 g, 8.4 mmoL) and water (20 mL) was added at room temperature, and stirred for 1 hour. The solvent of the reaction solution was distilled off under reduced pressure, and the residue was added with 6 N hydrochloric acid, and extracted with ethyl acetate, and washed with saturated brine. After drying over anhydrous magnesium sulfate, the solvent was distilled off, to give 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (0.73 g, yield: 74%).

¹H-NMR data (300 MHz, CDCl₃/TMS δ (ppm)): 1.03 (9H, s), 1.85 (2H, t), 4.15 (2H, t), 7.49 (1H, dd), 7.71 (1H, s), 8.23 (1H, d), 8.64 (1H, d), 9.04 (1H, d)

3) 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (Present Compound Number: A-0017)

In dichloromethane (15 mL), 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxylic acid (0.65 g, 2.3 mmoL) was dissolved, and oxalyl chloride (1 mL) and N,N-dimethylformamide (catalytic amount) were added, and heated under reflux at 40° C. for 1 hour. The solution was distilled off under reduced pressure, and the residue was suspended in THF (20 mL). After adding the solution to a mixed solution of THF (15 mL) and aqueous ammonia (content: 28%, 20 mL) under cooling on ice, the solution was stirred for 30 minutes under cooling on ice. The solvent of the reaction solution was distilled off under reduced pressure, and the residue was washed sequentially with water and hexane, and the obtained solid was dried, to give 4-(3,3-dimethylbutoxy)-1-(pyridine-3-yl)-1H-pyrazole-3-carboxamide (0.45 g, yield: 69%).

¹H-NMR data (300 MHz, CDCl₃/TMS δ (ppm)): 1.02 (9H, s), 1.83 (2H, t), 4.14 (2H, t), 5.73 (1H, br), 6.95 (1H, br), 7.42 (1H, dd), 7.67 (1H, s), 8.18 (1H, d), 8.58 (1H, d), 8.96 (1H, d)

Example 5 Production of N-isobutyryl-1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (Present Compound Number: A-2403)

In THF (10 mL), 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (0.40 g, 1.1 mmoL) was dissolved, and sodium hydride (content: 55%, 57 mg, 1.3 mmoL) was added under cooling on ice, and stirred for 30 minutes, and then isobutyric chloride (0.13 g, 1.2 mmoL) was added and stirred overnight at room temperature. Further, sodium hydride (content: 55%, 0.20 g, 4.6 mmoL) and isobutyric chloride (0.40 g, 3.8 mmoL) were added at room temperature, and stirred at 40° C. for 3 hours. After end of the reaction, 6 N hydrochloric acid was added so that the pH was 1 to 2, and then the solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography, to give N-isobutyryl-1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (0.21 g, yield: 44%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 1.26 (6H, d), 3.56 (1H, sext), 6.14 (1H, dt), 7.52 (1H, dd), 8.05-8.10 (2H, m), 8.71 (1H, dd), 9.00 (1H, d), 9.13 (1H, br)

Example 6 Production of 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carbonitrile

In dichloromethane (20 mL), 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (0.80 g, 2.2 mmoL) and triethylamine (0.66 g, 6.5 mmoL) were dissolved, and trifluoroacetic anhydride (0.57 g, 2.7 mmoL) was added under cooling on ice, and then the solution was stirred for 30 minutes, and then trifluoroacetic anhydride (0.10 g, 0.47 mmoL) was further added and stirred at room temperature for 30 minutes. After end of the reaction, the reaction solution was poured into water, and extracted with dichloromethane. The obtained organic layer was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography to 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carbonitrile (0.72 g, yield: 95%).

¹H-NMR data (400 MHz, CDCl₃/TMS δ (ppm)): 6.05 (1H, dt), 7.51 (1H, m), 8.06-8.10 (2H, m), 8.71 (1H, dd), 8.98 (1H, d)

Example 7 Production of 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carbothioamide (Present Compound Number: A-5436)

In 1,4-dioxane (10 mL), 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (0.60 g, 1.6 mmoL) was dissolved, and Lawesson's reagent (0.52 g, 1.3 mmoL) was added and stirred at 80° C. for 1 hour. After end of the reaction, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carbothioamide (0.64 g, yield: quantitative).

¹H-NMR data (400 MHz, DMSO-d6/TMS δ (ppm)): 7.17 (1H, dt), 7.61 (1H, dd), 8.37 (1H, d), 8.61 (1H, d), 8.96 (1H, s), 9.23 (1H, d), 9.53 (1H, br), 9.88 (1H, br)

Example 8 Production of 3-(3-carbamoyl-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-1-yl)pyridine-1-oxide (Present Compound Number: A-5510)

In chloroform (50 mL), 1-(pyridine-3-yl)-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-3-carboxamide (0.15 g, 0.4 mmoL) was dissolved, and m-chloroperbenzoic acid (content: 60%, 0.25 g, 0.87 mmoL) was added and heated under reflux for 1 hour. After end of the reaction, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography to give 3-(3-carbamoyl-4-[1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy]-1H-pyrazole-1-yl)pyridine 1-oxide (0.12 g, yield: 77%).

¹H-NMR data (400 MHz, DMSO-d6/TMS δ (ppm)): 7.24 (1H, d), 7.58 (2H, br), 7.93 (2H, br), 8.25 (1H, s), 9.01 (1H, d), 9.05 (1H, d)

Physical property values, including those in the above-described examples, of the present compound [I] synthesized in accordance with the above-described examples are shown in the following Table 150 to Table 155, and physical property values of the present compound [II] are similarly shown in the following Table 156 to Table 159. The compound numbers and the signs in Tables are as defined above.

TABLE 150 Compound Physical Property Value A-0001 Melting Point (° C.) 233-236 A-0002 Melting Point (° C.) 205-208 A-0003 Melting Point (° C.) 136-139 A-0005 Melting Point (° C.) 245-248 A-0006 Melting Point (° C.) 119-122 A-0007 Melting Point (° C.) 128-131 A-0008 Melting Point (° C.) 156-158 A-0009 Melting Point (° C.) 168-170 A-0010 Melting Point (° C.) 178-180 A-0011 Melting Point (° C.) 119-122 A-0012 Melting Point (° C.) 132-133 A-0013 Melting Point (° C.) 127-129 A-0014 Melting Point (° C.) 130-132 A-0015 Melting Point (° C.) 133-135 A-0016 Melting Point (° C.) 154-157 A-0017 Melting Point (° C.) 144-147 A-0018 Melting Point (° C.) 111-112 A-0019 Melting Point (° C.) 152-153 A-0020 Melting Point (° C.) 102-105 A-0021 Melting Point (° C.) 117-120 A-0022 Melting Point (° C.) 105-107 A-0028 Melting Point (° C.) 111-114 A-0031 Melting Point (° C.) 183-186 A-0032 Melting Point (° C.) 143-146 A-0034 Melting Point (° C.) 130-133 A-0043 Melting Point (° C.) 121-124 A-0044 Melting Point (° C.) 136-137 A-0045 Melting Point (° C.) 139-141 A-0046 Melting Point (° C.) 146-147 A-0047 Melting Point (° C.) 156-158 A-0050 Melting Point (° C.) 137-140 A-0051 Melting Point (° C.) 140-142 A-0052 Melting Point (° C.) 117-119 A-0056 Melting Point (° C.) 83-86 A-0058 Melting Point (° C.) 124-127 A-0060 Melting Point (° C.) 106-109 A-0061 Melting Point (° C.) 142-145 A-0062 Melting Point (° C.) 126-128 A-0065 Melting Point (° C.) 112-114 A-0067 Melting Point (° C.) 127-130 A-0070 Melting Point (° C.) 113-115 A-0071 Melting Point (° C.) 130-131 A-0072 Melting Point (° C.) 147-149 A-0073 Melting Point (° C.) 145-147 A-0075 Melting Point (° C.) 142-144 A-0076 Melting Point (° C.) 151-153 A-0077 Melting Point (° C.) 97-100 A-0078 Melting Point (° C.) 68-71 A-0080 Melting Point (° C.) 169-171 A-0081 Melting Point (° C.) 173-176 A-0082 Melting Point (° C.) 143-145 A-0083 Melting Point (° C.) 92-95 A-0086 Melting Point (° C.) 165-168

TABLE 151 Compound Physical Property Value A-0088 Melting Point (° C.)  99-102 A-0089 Melting Point (° C.) 173-175 A-0092 Melting Point (° C.) 151-154 A-0093 Melting Point (° C.) 151-154 A-0094 Melting Point (° C.) 147-150 A-0095 Melting Point (° C.) 188-191 A-0098 Melting Point (° C.) 131-133 A-0100 Melting Point (° C.) 90-93 A-0103 Melting Point (° C.) 160-163 A-0105 Melting Point (° C.) 151-152 A-0106 Melting Point (° C.) 65-68 A-0107 Melting Point (° C.) 96-97 A-0111 Refractive Index(n_(D) ²⁰) 1.6081 A-0113 Melting Point (° C.) 134-135 A-0120 Melting Point (° C.) 122-124 A-0121 Melting Point (° C.) 140-143 A-0122 Melting Point (° C.) 175-177 A-0124 Melting Point (° C.) 73-76 A-0125 Melting Point (° C.) 67-70 A-0126 Melting Point (° C.) 144-147 A-0134 Melting Point (° C.) 224-227 A-0135 Melting Point (° C.) 164-166 A-0136 Melting Point (° C.) 164-166 A-0137 Melting Point (° C.) 256-259 A-0138 Melting Point (° C.) 184-187 A-0144 Melting Point (° C.) 118-121 A-0145 Melting Point (° C.) 136-139 A-0151 Melting Point (° C.) 101-103 A-0152 Melting Point (° C.) 86-89 A-0153 Melting Point (° C.) 115-118 A-0165 Melting Point (° C.) 96-98 A-0166 Melting Point (° C.) 102-104 A-0177 Melting Point (° C.) 210-213 A-0186 Melting Point (° C.) 170-173 A-0192 Melting Point (° C.) 160-163 A-0197 Melting Point (° C.) 200-203 A-0199 Melting Point (° C.) 180-183 A-0203 Melting Point (° C.) 195-198 A-0205 Melting Point (° C.) 210-213 A-0211 Melting Point (° C.) 172-175 A-0212 Melting Point (° C.) 191-194 A-0217 Melting Point (° C.) 188-191 A-0221 Melting Point (° C.) 120-123 A-0225 Melting Point (° C.) 166-168 A-0234 Melting Point (° C.) 153-156 A-0240 Melting Point (° C.) 162-165 A-0246 Melting Point (° C.) 157-160 A-0247 Melting Point (° C.) 158-161 A-0248 Melting Point (° C.) 147-149 A-0249 Melting Point (° C.) 175-178 A-0253 Melting Point (° C.) 67-70 A-0254 Melting Point (° C.) 149-152 A-0283 Melting Point (° C.) 53-56

TABLE 152 Compound Physical Property Value A-0468 Melting Point (° C.) 91-92 A-0658 Melting Point (° C.)  99-101 A-0849 Melting Point (° C.) 94-97 A-1045 Melting Point (° C.) 104-106 A-1106 Melting Point (° C.) 57-60 A-1120 Refractive Index(n_(D) ²⁰) 1.5054 A-1302 Melting Point (° C.) 83-86 A-1368 Refractive Index(n_(D) ²⁰) 1.4932 A-1429 Melting Point (° C.) 78-81 A-1625 Melting Point (° C.) 123-125 A-1684 Melting Point (° C.) 125-128 A-1882 Melting Point (° C.) 125-127 A-1948 Refractive Index(n_(D) ²⁰) 1.5037 A-2014 Melting Point (° C.) 92-95 A-2080 Melting Point (° C.) 129-131 A-2155 Melting Point (° C.) 174-177 A-2164 Melting Point (° C.) 190-193 A-2337 Melting Point (° C.) 141-143 A-2403 Refractive Index(n_(D) ²⁰) 1.4956 A-2469 Melting Point (° C.) 159-162 A-2535 Refractive Index(n_(D) ²⁰) 1.4759 A-2610 Melting Point (° C.) 66-69 A-2792 Melting Point (° C.)  99-102 A-2858 Melting Point (° C.) 111-114 A-2924 Melting Point (° C.) 102-105 A-2990 Melting Point (° C.) 127-129 A-3056 Melting Point (° C.) 142-145 A-3122 Melting Point (° C.) 124-126 A-3188 Melting Point (° C.)  99-100 A-3254 Melting Point (° C.) 135-137 A-3320 Melting Point (° C.) 165-167 A-3386 Refractive Index(n_(D) ²⁰) 1.4935 A-3518 Refractive Index(n_(D) ²⁰) 1.4962 A-3584 Melting Point (° C.) 145-149 A-3650 Refractive Index(n_(D) ²⁰) 1.5076 A-3716 Refractive Index(n_(D) ²⁰) 1.5279 A-3791 Refractive Index(n_(D) ²⁰) 1.4919 A-3973 Melting Point (° C.) 92-95 A-4095 Melting Point (° C.) 113-115 A-4257 Melting Point (° C.) 173-175 A-4304 Melting Point (° C.) 103-104 A-4883 Melting Point (° C.) 171-174 A-5436 Melting Point (° C.) 155-158 A-5510 Melting Point (° C.) 207-210

TABLE 153 Compound Physical Property Value Methanesulfonate of A-0050 Melting Point (° C.) 168-170 Methanesulfonate of A-0071 Melting Point (° C.) 137-140 p-toluenespifonate of A-0071 Melting Point (° C.) 127-130 Hydrochloride of A-0071 Melting Point (° C.) 139-142

TABLE 154 Compound Physical Property Value (¹H-NMR Data, in CDCl₃ TMS δ(ppm)) A-0027 300 MHz 1.24(3H, t), 3.60(2H, q), 3.82(2H, t), 4.26 (2H, t), 6.32(1H, br), 7.08(1H, br), 7.43(1H, dd), 7.79 (1H, s),8.18(1H, d), 8.59(1H,d), 8.97(1H,d) A-0209 300 MHz 1.71(3H, d), 3.84-4.01(2H, m), 4.58(1H, q), 5.84(1H, br), 6.84(1H, br), 7.42(1H, br), 7,82 (1H, s), 8.00(1H, d), 8.68(1H, br), 8.99(2H,br) A-1443 300 MHz 4.12(2H, m), 6.11(1H, dt), 7.11(1H, br), 7.49 (1H, dd),8.04-8.08(2H, m), 8.69(1H, dd), 9.00 (1H, d) A-1686 400 MHz 4.41(2H, d), 4.72(2H, t), 7.29(1H, br), 7.52 (1H, dd),7.85(1H, s), 8.03(1H, d), 8.65(1H,d), 8.97(1H,d) A-2139 400 MHz 2.62(3H, s), 5.20(1H, dsext), 7.52(1H, dd), 8.06-8.09(2H, m), 8.71(1H, dd), 8.99(1H, d), 9.21 (1H, br) A-3452 400 MHz 1.82(4H, quin), 2.73(4H, quin), 4.38-4.47 (2H, m),6.18(1H, dt), 7.27(1H, br), 7.45-7.49 (1H, m), 8.02-8.07(2H, m), 8.66(1H, dd), 9.00 (1H, d) A-4038 300 MHz 3.77-3.84(8H, m), 6.05(1H, dt), 7.45(1H, dd), 8.01-8.05(2H, m), 8.64(1H, dd), 8.97(1H, d) A-5658 300 MHz 2.66-2.83(2H, m), 4.42(2H, t), 5,66(1H, br), 6.81(1H, br), 7.45(1H, dd), 7.73(1H, s), 8.13 (1H, m), 8.61(1H, dd), 8.97(1H, d) Compound Physical Property Value (¹H-NMR Data, DMSO-d₆ TMS δ(ppm)) A-0004 400 MHz 1.33(6H, d), 4.44(1H, sep), 7.29(1H, br), 7.52 (1H, br), 7.57(1H, dd), 8.30(1H, dd), 8.54 (1H, dd), 8.59(1H, s), 9.16(1H,d)

TABLE 155 Physical Property Value(HRMS, m/z ([M + H])) Compound Chemical Formula Calculated Value Measured Value A-1700 C₁₄H₁₉ F₆N₅O₃ 410.0688 410.0694

TABLE 156 Compound Physical Property Value B-0003 Melting Point (° C.) 240-243 B-0004 Melting Point (° C.) 217-220 B-0006 Melting Point (° C.) 199-202 B-0007 Melting Point (° C.) 168-170 B-0008 Melting Point (° C.) 163-164 B-0009 Melting Point (° C.) 144-147 B-0010 Melting Point (° C.) 212-215 B-0011 Melting Point (° C.) 133-134 B-0013 Melting Point (° C.) 162-164 B-0014 Melting Point (° C.) 150-153 B-0015 Melting Point (° C.) 145-148 B-0016 Melting Point (° C.) 150-153 B-0017 Melting Point (° C.) 165-168 B-0019 Melting Point (° C.) 176-178 B-0020 Melting Point (° C.) 157-158 B-0021 Melting Point (° C.) 151-154 B-0022 Melting Point (° C.) 147-150 B-0043 Melting Point (° C.) 177-180 B-0045 Melting Point (° C.) 165-168 B-0046 Melting Point (° C.) 207-210 B-0050 Melting Point (° C.) 174-176 B-0051 Melting Point (° C.) 159-161 B-0052 Melting Point (° C.) 170-173 B-0056 Melting Point (° C.) 138-141 B-0058 Melting Point (° C.) 177-180 B-0062 Melting Point (° C.) 171-174 B-0065 Melting Point (° C.) 164-167 B-0067 Melting Point (° C.) 167-170 B-0068 Melting Point (° C.) 201-204 B-0075 Melting Point (° C.) 173-175 B-0078 Melting Point (° C.) 126-129 B-0080 Melting Point (° C.) 225-228 B-0081 Melting Point (° C.) 213-215 B-0082 Melting Point (° C.) 211-213 B-0083 Melting Point (° C.) 200-202 B-0088 Melting Point (° C.) 181-183 B-0089 Melting Point (° C.) 168-171 B-0093 Melting Point (° C.) 210-213 B-0094 Melting Point (° C.) 193-196 B-0095 Melting Point (° C.) 215-217 B-0098 Melting Point (° C.) 166-169 B-0100 Melting Point (° C.) 153-155 B-0103 Melting Point (° C.) 182-185 B-0105 Melting Point (° C.) 175-178 B-0120 Melting Point (° C.) 131-133 B-0121 Melting Point (° C.) 179-181 B-0136 Melting Point (° C.) 136-139 B-0137 Melting Point (° C.) 166-168 B-0151 Melting Point (° C.) 182-185 B-0152 Melting Point (° C.) 166-169 B-0153 Melting Point (° C.) 142-144 B-0165 Melting Point (° C.) 120-123 B-0166 Melting Point (° C.) 145-147

TABLE 157 Compound Physical Property Value B-0192 Melting Point (° C.) 248-249 B-0246 Melting Point (° C.) 250-253 B-0247 Melting Point (° C.) 230-233 B-0248 Melting Point (° C.) 207-209 B-0249 Melting Point (° C.) 200-203 B-0253 Melting Point (° C.) 189-192 B-0254 Melting Point (° C.) 218-221 B-0255 Melting Point (° C.) 130-131 B-0256 Melting Point (° C.) 130-133 B-0257 Melting Point (° C.) 104-106 B-0258 Refractive Index(n_(D) ²⁰) 1.5569 B-0259 Refractive Index(n_(D) ²⁰) 1.5322 B-0260 Melting Point (° C.) 95-96 B-0261 Melting Point (° C.) 105-107 B-0263 Melting Point (° C.) 59-62 B-0264 Melting Point (° C.) 87-90 B-0265 Melting Point (° C.) 122-125 B-0266 Melting Point (° C.) 90-91 B-0267 Melting Point (° C.) 92-95 B-0268 Refractive Index(n_(D) ²⁰) 1.551 B-0269 Melting Point (° C.) 80-82 B-0271 Melting Point (° C.) 91-92 B-0272 Melting Point (° C.) 57-60 B-0273 Melting Point (° C.) 61-63 B-0274 Melting Point (° C.) 51-53 B-0275 Melting Point (° C.) 50-52 B-0276 Melting Point (° C.) 47-50 B-0281 Melting Point (° C.) 73-74 B-0282 Melting Point (° C.) 41-43 B-0285 Melting Point (° C.) 94-97 B-0286 Melting Point (° C.) 103-104 B-0298 Melting Point (° C.) 101-102 B-0299 Melting Point (° C.) 125-127 B-0300 Melting Point (° C.) 73-76 B-0304 Melting Point (° C.) 103-104 B-0305 Melting Point (° C.) 124-126 B-0306 Melting Point (° C.) 117-120 B-0310 Melting Point (° C.) 96-99 B-0312 Melting Point (° C.) 97-99 B-0314 Melting Point (° C.) 63-65 B-0316 Melting Point (° C.) 110-112 B-0319 Melting Point (° C.) 104-107 B-0321 Melting Point (° C.) 80-83 B-0324 Melting Point (° C.) 94-97 B-0325 Melting Point (° C.) 85-87 B-0329 Melting Point (° C.)  97-100 B-0330 Melting Point (° C.) 126-128 B-0332 Melting Point (° C.) 108-110 B-0334 Melting Point (° C.) 122-124 B-0335 Melting Point (° C.) 107-109 B-0336 Refractive Index(n_(D) ²⁰) 1.5509 B-0340 Melting Point (° C.) 124-127 B-0342 Melting Point (° C.) 66-68

TABLE 158 Compound Physical Property Value B-0343 Melting Point (° C.)  98-101 B-0346 Melting Point (° C.) 103-106 B-0347 Melting Point (° C.) 105-106 B-0348 Melting Point (° C.) 96-98 B-0349 Melting Point (° C.) 118-120 B-0352 Melting Point (° C.) 95-96 B-0354 Melting Point (° C.) 88-90 B-0357 Melting Point (° C.)  98-101 B-0359 Melting Point (° C.) 123-125 B-0360 Melting Point (° C.) 102-103 B-0361 Melting Point (° C.) 86-87 B-0367 Melting Point (° C.) 65-66 B-0374 Melting Point (° C.) 55-58 B-0375 Refractive Index(n_(D) ²⁰) 1.5681 B-0376 Melting Point (° C.) 143-146 B-0378 Melting Point (° C.) 114-116 B-0379 Melting Point (° C.) 118-119 B-0380 Melting Point (° C.) 80-82 B-0390 Melting Point (° C.) 115-117 B-0405 Melting Point (° C.) 110-113 B-0406 Melting Point (° C.) 97-99 B-0407 Melting Point (° C.) 91-94 B-0419 Melting Point (° C.) 63-66 B-0420 Melting Point (° C.) 57-60 B-0438 Melting Point (° C.) 136-138 B-0446 Melting Point (° C.) 90-92 B-0463 Melting Point (° C.) 158-161 B-0465 Melting Point (° C.)  97-100 B-0471 Melting Point (° C.) 103-106 B-0475 Melting Point (° C.) 138-141 B-0494 Melting Point (° C.) 129-130 B-0500 Melting Point (° C.) 153-156 B-0501 Melting Point (° C.) 93-95 B-0502 Melting Point (° C.) 165-167 B-0503 Melting Point (° C.) 160-162 B-0504 Melting Point (° C.) 159-161 B-0507 Refractive Index(n_(D) ²⁰) 1.5858 B-0508 Melting Point (° C.) 115-117 B-0891 Melting Point (° C.) 90-93 B-1088 Melting Point (° C.) 121-122 B-1133 Melting Point (° C.) 53-54 B-1474 Melting Point (° C.) 129-131 B-1667 Melting Point (° C.) 141-143 B-2107 Melting Point (° C.) 196-199 B-2246 Melting Point (° C.) 122-124 B-2300 Melting Point (° C.) 108-109

TABLE 159 Compound Physical Property Value (¹H-NMR Data, in CDCl₃ TMS δ(ppm)) B-0262 300 MHz 1.02(3H, t), 1.37-1,45(6H, m), 1.66-1.84 (2H, m),4.08-4.18(1H, m), 4.40-4.49(2H, m), 7.42(1H, dd), 7.62(1H, s), 8.11-8.15(1H, m), 8.59(1H, dd), 8.95(1H,d) B-0270 300 MHz 0.93-1.03(6H, m), 1.40-1.82(9H, m), 3.92-3.99 (1H,m), 4.42(2H, q), 7,39-7.44(1H, m), 7.58 (1H, s), 8.11-8.15(1H, m), 8.58(1H, dd), 8.94 (1H, d) B-0297 300 MHz 1.43(3H, t), 2.64-2.77(2H, m), 4.26(2H, t), 4.45(2H,q), 7.44(1H, dd), 7.70(1H, s), 8.11- 8.15(1H, m), 8.61(1H, d), 8.96(1H, d) B-0337 300 MHz 0.65-0.81(4H, m), 1.22-1.30(1H, m), 1.41 (3H, t), 4.44(2H, q), 4.70(2H, d), 7.42(1H, dd), 7.78(1H, s), 8.10-8.15(1H, m), 8.59(1H, dd), 8,94(1H, d) B-0702 400 MHz 1.41(3H, t), 4.51(2H, t), 7.37(1H, br), 7.46 (1H, s),7.70(1H, d), 8,86(1H, s), 8.92(1H, d) B-0727 400 MHz 1.40(3H, t), 4.49(2H, q), 4.63(1H, t), 7,60 (1H, s),7.74(1H, d), 8.90(1H, s), 8.92(1H, d) B-3247 400 MHz 7.29(1H, dt), 7.59(1H, dd), 7.89(1H, dd), 8.27(1H, d),8.91(1H, t), 9.04(1H, s), 13.52 (1H, br) B-3322 300 MHz 1.41(3H, t), 4.45(2H, q), 6.04(1H, dt), 7.41 (1H, dd),7.68(1H, dd), 7.98(1H, s), 8.21 (1H, d), 8.76(1H, t) B-3361 300 MHz 1.43(3H, t), 2.65-2.82(2H, m), 4.34(2H, t), 4,45(2H, q), 7.44(1H, dd), 7.71(1H, s), 8.11- 8.15(1H, m), 8.62(1H, dd), 8.96(1H, d)

Next, formulation examples of the harmful organism control agent of the present invention using the pyrazole-3-carboxylic acid amide derivative of the present invention produced in the manner as described above, or an agriculturally acceptable salt thereof will be specifically described. It is to be noted that the compound, the kinds and the mixing ratios of additives are not limited to this, but may be changed in a wide range. In the following description, “part” means a part by mass.

(Formulation Example 1) Emulsion

Compounds described in Table 1 to 10 parts Table 93, and Table 150 to Table 155 cyclohexanone 30 parts Polyoxyethylene alkyl aryl ether 11 parts Sodium alkylbenzenesulfonate  4 parts Methylnaphthalene 45 parts

These ingredients were uniformly dissolved to give an emulsifiable concentrate.

(Formulation Example 2) Water-Dispersible Powder

Compounds described in Table 1 to  10 parts Table 93, and Table 150 to Table 155 Sodium salt of naphthalene sulfonic 0.5 parts acid formalin condensate Polyoxyethylene alkyl aryl ether 0.5 parts Diatomaceous earth  24 parts Clay  65 parts

These ingredients were uniformly mixed and ground to give a water-dispersible powder.

(Formulation Example 3) Dust

Compounds described in Table 1 to  2 parts Table 93, and Table 150 to Table 155 Diatomaceous earth  5 parts Clay 93 parts

These ingredients were uniformly mixed and ground to give a dust.

(Formulation Example 4) Granule

Compounds described in Table 1 to  5 parts Table 93, and Table 150 to Table 155 Sodium salt of lauryl alcohol sulfate  2 parts Sodium ligninsulfonate  5 parts Carboxymethylcellulose  2 parts Clay 86 parts

These ingredients were uniformly mixed and ground. To this mixture, water in an amount corresponding to 20 parts was added and kneaded, and processed into 14 to 32 mesh granules by using an extruding granulator, and then dried to give granules.

(Formulation Example 5) Flowable Concentrate

Compounds described in Table 1 to   20 parts Table 93, and Table 150 to Table 155 Polyoxyethylene styrenated phenyl    4 parts ether sulfate Ethylene glycol    7 parts Silicone AF-118N (available from  0.02 parts Asahi Kasei Corporation) Water 68.98 parts

These ingredients were mixed with a high-speed stirrer for 30 minutes, and then ground with a wet grinder to give a flowable concentrate.

(Formulation Example 6) Water-Dispersible Granule

Compounds described in Table 1 to 10 parts Table 93, and Table 150 to Table 155 Sodium ligninsulfonate  5 parts Polyoxyethylene alkyl aryl ether  1 part Sodium polycarboxylate  3 parts White carbon  5 parts Pregelatinized starch  1 part Calcium carbonate 65 parts Water 10 parts

These ingredients were mixed and kneaded and extrusion granulated. The obtained granules were dried by a fluidized-bed dryer, to give a water-dispersible granule.

Next, the effect exerted by the harmful organism control agent of the present invention will be described by way of test examples.

(Test Example 1) Plutella xylostella Killing Test

The water-dispersible powder prepared in accordance with Manufacturing example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A cabbage leaf was dipped in this liquid agent, and air-dried, and then put into a plastic cup. Ten second instar larvae of Plutella xylostella were released in the cup, and the cup was lidded. Then, the cup was placed in a thermostatic chamber at 25° C., and the number of dead insects was examined after 6 days, and the percentage of dead insects was determined by the calculation formula of numerical formula 1. The test was conducted singly.

$\begin{matrix} {{{Percentage}\mspace{14mu} {of}\mspace{14mu} {Dead}\mspace{14mu} {{Insects}(\%)}} = {\left( {- \frac{{Number}\mspace{14mu} {of}\mspace{14mu} {Live}\mspace{14mu} {Insects}}{{Number}\mspace{14mu} {of}\mspace{14mu} {tested}\mspace{14mu} {Insects}}} \right) \times 100}} & \left\lbrack {{Numerical}\mspace{14mu} {formula}\mspace{14mu} 1} \right\rbrack \end{matrix}$

The compounds showing a percentage of dead insects of 50% or more in this test are as follows.

A-0001, A-0006, A-0008A, A-0009, A-0010, A-0015, A-0015, A-0028, A-0067, A-0082, A-0083, A-0098, A-0100, A-0111, A-0120, A-0125, A-0144, A-0145, A-0165, A-0177, A-0197, A-0203, A-0211, A-0212, A-0225, A-0234, A-0246, A-0247, A-0248, A-0254, A-0283, A-1106, A-1120, A-1302, A-1368, A-1429, A-1443, A-1684, A-1948, A-2014, A-2164, A-2337, A-2403, A-2469, A-2535, A-2610, A-2858, A-2924, A-2990, A-3056, A-3188, A-3254, A-3320, A-3386, A-3452, A-3518, A-3584, A-3650, A-3716, A-3791, A-3973, A-4257, B-0006, B-0009, B-0010, B-0013, B-0014, B-0015, B-0016, B-0017, B-0043, B-0050, B-0051, B-0068, B-0083, B-0093, B-0098, B-0100, B-0137, B-0246, B-0247, B-0253, B-0254, B-0263, B-0264, B-0267, B-0269, B-0270, B-0271, B-0275, B-0285, B-0286, B-0332, B-0336, B-0337, B-0347, B-0354, B-0357, B-0360, B-0374, B-0375, B-0376, B-0379, B-0405, B-0438, B-0446, B-0465, B-0500, B-0503, B-0507, B-0508, B-0727, B-01088, B-01474, B-02300

(Test Example 2) Helicoverpa armigera Killing Test

The water-dispersible powder prepared in accordance with Manufacturing example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A cabbage leaf was dipped in this liquid agent, and air-dried, and then put into a plastic cup. Five newly hatched larvae of Helicoverpa armigera were released in the cup, and the cup was lidded. Then, the cup was placed in a thermostatic chamber at 25° C., and the number of dead insects was examined after 6 days, and the percentage of dead insects was determined by the calculation formula of numerical formula 1. The test was conducted in duplicate.

The compounds showing a percentage of dead insects of 50% or more in this test are as follows.

A-0004, A-0006, A-0018, A-0043, A-0045, A-0052, A-0058, A-0061, A-0062, A-0065, A-0067, A-0073, A-0145, A-0151, A-0186, A-0246, A-1106, A-1429, A-1443, A-1625, A-3122, A-3254, A-3320, A-3791, A-3973, A-4257, A-4304, A-5436, B-0004, B-0006, B-0016, B-0043, B-0045, B-0056, B-0065, B-0067, B-0088, B-0089, B-0095, B-0153, B-0165, B-0192, B-0246, B-0256, B-0276, B-02786, B-0297, B-0299, B-0300, B-0312, B-0316, B-0319, B-0321, B-0334, B-0340, B-0348, B-0349, B-0360, B-0405, B-0407, B-0471, B-0475, B-0500, B-0508, B-0891, B-1133, B-1667, B-2300

(Test Example 3) Aphis gossypii Killing Test

The water-dispersible powder prepared in accordance with Formulation example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. A nursery plant of cucumber preliminarily inoculated with nymphs of Aphis gossypii was dipped in this liquid agent, and air-dried. The nursery plant of cucumber after the treatment was placed in a thermostatic chamber at 25° C., and the number of live insects was counted after 3 days, and the percentage of dead insects was determined by the calculation formula of numerical formula 1. The test was conducted singly.

The compounds showing a percentage of dead insects of 50% or more in this test are as follows.

A-0001, A-0002, A-0003, A-0004, A-0005, A-0006, A-0007, A-0008, A-0009, A-0010, A-0011, A-0012, A-0013, A-0014, A-0015, A-0017, A-0018, A-0019, A-0020, A-0027, A-0028, A-0031, A-00, A-0034, A-0043, A-0044, A-0045, A-0046, A-0047, A-0050, A-0051, A-0052, A-0053, A-0056, A-0058, A-0060, A-0061, A-0062, A-0065, A-0067, A-0070, A-0071, A-0072, A-0073, A-0075, A-0076, A-0077, A-0078, A-0080, A-0081, A-0083, A-0086, A-0088, A-0092, A-0093, A-0094, A-0098, A-0100, A-0103, A-0105, A-0106, A-0111, A-0113, A-0122, A-0151, A-0152, A-0153, A-0165, A-0186, A-0221, A-0225, A-0234, A-0240, A-0249, A-0253, A-0254, A-0283, A-0468, A-0658, A-0849, A-1045, A-1106, A-1120, A-1302, A-1368, A-1429, A-1443, A-1625, A-1684, A-1686, A-1700, A-1882, A-1948, A-2014, A-2080, A-2155, A-2164, A-2337, A-2403, A-2469, A-2535, A-2610, A-2792, A-2858, A-2924, A-2990, A-3056, A-3122, A-3188, A-3254, A-3320, A-3386, A-3452, A-3518, A-3584, A-3650, A-3716, A-3791, A-3973, A-4095, A-4304, A-5436, A-5510

(Test Example 4) Nilaparvata lugens Killing Activity Test

The water-dispersible powder prepared in accordance with Formulation example 2 was diluted in water so that the concentration of the active ingredient was 500 ppm. Paddy was dipped in this liquid agent, and then put into a plastic cup. Ten second instar larvae of Nilaparvata lugens were released in the plastic cup, and the cup was lidded, and placed in a thermostatic chamber at 25° C. After 6 days, the number of live insects was counted, and the percentage of dead insects was determined by the calculation formula of numerical formula 1. The test was conducted singly.

The compounds showing a percentage of dead insects of 50% or more in this test are as follows.

A-0002, A-0003, A-0004, A-0005, A-0006, A-0007, A-0009, A-0010, A-0011, A-0013, A-0015, A-0016, A-0017, A-0018, A-0019, A-0020, A-0021, A-0022, A-27, A-0028, A-0032, A-0034, A-0043, A-0045, A-0046, A-0047, A-0051, A-0052, A-0056, A-0058, A-0060, A-0062, A-0067, A-0070, A-0071, A-0073, A-0075, A-0076, A-0078, A-0080, A-0081, A-0081, A-0082, A-0083, A-0089, A-0092, A-0093, A-0094, A-0095, A-0098, A-0100, A-0103, A-0105, A-0113, A-0120, A-0121, A-01222, A-0125, A-0126, A-0135, A-0136, A-0137, A-0144, A-0145, A-0151, A-0153, A-0165, A-0166, A-0177, A-0186, A-0209, A-0211, A-0217, A-0221, A-0234, A-0246, A-0247, A-0248, A-0249, A-0253, A-0254, A-0283, A-0468, A-0658, A-1045, A-1106, A-1120, A-1368, A-1443, A-1625, A-1684, A-1700, A-1882, A-1948, A-2014, A-2080, A-2155, A-2164, A-2337, A-2403, A-2469, A-2990, A-3056, A-3122, A-3188, A-3320, A-3386, A-3452, A-3518, A-3584, A-3650, A-3973, A-4095, A-4257, A-5436, A-5510, B-0004, B-0009, B-0010, B-0011, B-0015, B-0016, B-0017, B-0021, B-0022, B-0045, B-0046, B-0058, B-0062, B-0067, B-0075, B-0081, B-0082, B-0083, B-0093, B-0100, B-0105, B-0121, B-0151, B-0257, B-0258, B-0259, B-0260, B-0262, B-0263, B-0264, B-0265, B-0268, B-0269, B-0270, B-0271, B-0273, B-0274, B-0275, B-0276, B-0285, B-0286, B-0297, B-0299, B-0300, B-0305, B-0306, B-0312, B-0314, B-0316, B-0329, B-0332, B-0336, B-0337, B-0342, B-0352, B-0354, B-0357, B-0359, B-0361, B-0367, B-0374, B-0375, B-0378, B-0379, B-0380, B-0390, B-0405, B-0407, B-0419, B-0420, B-0463, B-0465, B-0507, B-0727, B-1133

INDUSTRIAL APPLICABILITY

The present invention provides a novel compound having excellent insecticide activity, and is useful in pesticide fields and agricultural fields, and has industrial applicability. 

1. A pyrazole-3-carboxylic acid amide derivative represented by general formula [I] or an agriculturally acceptable salt thereof:

wherein, n represents an integer of 0 or 1, X represents an oxygen atom or a sulfur atom, R¹, R², R³, R⁴, and R⁵ each independently represent a hydrogen atom, halogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkoxy group, C₃-C₆ cycloalkyl group, C₁-C₆ alkylthio group, C₁-C₆ alkylsulfinyl group, C₁-C₆ alkylsulfonyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, cyano group, or nitro group, R⁶ represents a hydrogen atom, C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹, R⁷ and R⁸ each independently represent a hydrogen atom, C₁-C₆ alkyl group, C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₂-C₇ alkynyl group, C₂-C₆ alkenyl group, hydroxy group, C₁-C₆ alkoxy group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, 2-tetrahydrofuranyl group, 3-tetrahydrofuranyl group, 2-tetrahydropyranyl group, 4-tetrahydropyranyl group, cyano C₁-C₆ alkyl group, cyano C₃-C₆ cycloalkyl group, hydroxy C₁-C₆ alkyl group, formyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, C₁-C₆ alkylcarbonyl group, C₁-C₆ alkoxy C₁-C₆ alkylcarbonyl group, C₃-C₆ cycloalkyl carbonyl group, C₃-C₆ cycloalkyl C₁-C₆ alkylcarbonyl group, C₁-C₆ alkoxycarbonyl group, carbamoyl group, mono(C₁-C₆ alkyl)aminocarbonyl group, di(C₁-C₆ alkyl)aminocarbonyl group, phenylcarbonyl group that is unsubstituted or substituted with R⁹, C₇-C₁₃ aralkylcarbonyl group that is unsubstituted or substituted with R⁹, pyridylcarbonyl group that is unsubstituted or substituted with R⁹, pyrazolylcarbonyl group that is unsubstituted or substituted with R⁹, (C₁-C₆ alkyl)thiocarbonyl group, (C₁-C₆ alkoxy)thiocarbonyl group, thiocarbamoyl group, mono(C₁-C₆ alkyl)aminothiocarbonyl group, di(C₁-C₆ alkyl)aminothiocarbonyl group, C₁-C₆ alkylsulfonyl group, sulfamoyl group, mono(C₁-C₆ alkyl)aminosulfonyl group, di(C₁-C₆ alkyl)aminosulfonyl group, R¹⁰R¹¹N—C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, hydroxyimino group, C₁-C₆ alkoxyimino group, hydroxyimino C₁-C₆ alkyl group, or C₁-C₆ alkoxyimino C₁-C₆ alkyl group, and R⁷ and R⁸ may together form ═CR¹²N(R¹³)R¹⁴ or ═CR¹²OR¹⁵, and R⁷ and R⁸ may form, together with a carbon atom bound thereto, a 3 to 6-membered carbon ring, or a 3 to 6-membered hetero ring having 1 to 4 heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and the hetero ring may be substituted with a halogen atom, cyano group, nitro group, C₁-C₆ alkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkyl group, or oxo group, R⁹ represents a halogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkoxy group, C₁-C₆ alkylthio group, C₁-C₆ alkylsulfinyl group, C₁-C₆ alkylsulfonyl group, C₁-C₆ haloalkylthio group, C₁-C₆ haloalkylsulfinyl group, C₁-C₆ haloalkylsulfonyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, cyano group, or nitro group, R¹⁰ and R¹¹ each independently represent a hydrogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, or C₃-C₆ cycloalkyl group, and R¹⁰ and R¹¹ may form, together with a carbon atom bound thereto, a 3 to 6-membered ring, R¹² represents a hydrogen atom, C₁-C₆ alkyl group, or C₃-C₆ cycloalkyl group, R¹³ and R¹⁴ each independently represent a hydrogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₃-C₆ cycloalkyl group, or C₁-C₆ alkoxy group, and R¹³ and R¹⁴ may form, together with a carbon atom bound thereto, a 3 to 6-membered carbon ring, or a 3 to 6-membered hetero ring having 1 to 4 heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and R¹⁵ represents a C₁-C₆ alkyl group.
 2. A pyrazole-3-carboxylic acid derivative represented by general formula [II] or a salt thereof:

wherein, n represents an integer of 0 or 1, R¹, R², R³, R⁴, and R⁵ each independently represent a hydrogen atom, halogen atom, C₁-C₆ alkyl group, C₁-C₆ haloalkyl group, C₁-C₆ alkoxy group, C₁-C₆ haloalkoxy group, C₃-C₆ cycloalkyl group, C₁-C₆ alkylthio group, C₁-C₆ alkylsulfinyl group, C₁-C₆ alkylsulfonyl group, amino group, mono(C₁-C₆ alkyl)amino group, di(C₁-C₆ alkyl)amino group, cyano group, or nitro group, R⁶ represents a hydrogen atom, C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl sulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹, and R¹⁶ represents a hydrogen atom or C₁-C₆ alkyl group.
 3. A pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim 1, wherein R⁶ represents a C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹.
 4. A pyrazole-3-carboxylic acid derivative or a salt thereof according to claim 2, wherein R⁶ represents a C₁-C₁₂ alkyl group, C₁-C₆ alkoxy C₁-C₆ alkyl group, C₁-C₁₂ haloalkyl group, C₁-C₆ alkoxy C₁-C₆ haloalkyl group, C₁-C₆ haloalkoxy C₁-C₆ alkyl group, C₁-C₆ haloalkoxy C₁-C₆ haloalkyl group, C₂-C₇ alkynyl group, C₃-C₆ cycloalkyl C₂-C₆ alkynyl group, C₂-C₆ haloalkynyl group, C₂-C₆ alkenyl group, C₂-C₆ haloalkenyl group, C₃-C₆ cycloalkyl group, C₃-C₆ halocycloalkyl group, C₁-C₆ haloalkyl C₃-C₆ cycloalkyl group, C₃-C₆ cycloalkyl C₁-C₆ alkyl group, C₃-C₆ halocycloalkyl C₁-C₆ alkyl group, C₁-C₆ alkylthio C₁-C₆ alkyl group, C₁-C₆ alkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ alkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylthio C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfinyl C₁-C₆ alkyl group, C₁-C₆ haloalkylsulfonyl C₁-C₆ alkyl group, C₁-C₆ alkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ haloalkylcarbonyl C₁-C₆ alkyl group, C₁-C₆ alkoxycarbonyl C₁-C₆ alkyl group, aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₃-C₆ cycloalkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ haloalkyl)aminocarbonyl C₁-C₆ alkyl group, di(C₁-C₆ alkyl)aminocarbonyl C₁-C₆ alkyl group, mono(C₁-C₆ alkylcarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkoxycarbonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ alkylsulfonyl)amino C₁-C₆ alkyl group, mono(C₁-C₆ haloalkylsulfonyl)amino C₁-C₆ alkyl group, hydroxy C₁-C₆ alkyl group, hydroxyimino C₁-C₆ alkyl group, C₁-C₆ alkoxyimino C₁-C₆ alkyl group, C₁-C₆ haloalkoxyimino C₁-C₆ alkyl group, or C₇-C₁₃ aralkyl group that is unsubstituted or substituted with R⁹.
 5. A pesticide composition containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 1. 6. A pesticide composition according to claim 5, wherein the pesticide composition further contains a surfactant.
 7. A harmful organism control agent containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 1. 8. A harmful organism control agent according to claim 7 that is an insecticide.
 9. A harmful organism control agent according to claim 7 having a control effect on a harmful organism in a dry field or a paddy field where a farming or gardening plant is cultured.
 10. A harmful organism control agent according to claim 9, wherein the farming or gardening plant is a plant provided with tolerance by a breeding method or a gene recombination technique.
 11. A method for controlling a harmful organism using an active ingredient amount of the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 1. 12. A method for controlling a harmful organism by letting a pesticide composition containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 1. 13. A method for controlling a harmful organism according to claim 11, wherein the place where the harmful organism control agent is to be applied is a paddy field, a dry field, a lawn, an orchard, a non-crop land, a greenhouse, a raising seeding facility, or a plant factory.
 14. A method for controlling a harmful organism according to any one of claim 11, wherein the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof is used as an insecticide.
 15. A use method of a harmful organism control agent, using the harmful organism control agent according to claim 7 for controlling a harmful organism for a farming or gardening crop.
 16. A pesticide composition containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 3. 17. A pesticide composition containing the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim 2 as an active ingredient.
 18. A pesticide composition containing the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim 4 as an active ingredient.
 19. A pesticide composition according to claim 17, wherein the pesticide composition further contains a surfactant.
 20. A harmful organism control agent containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 3. 21. A harmful organism control agent containing the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim 2 as an active ingredient.
 22. A harmful organism control agent containing the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim 4 as an active ingredient.
 23. The harmful organism control agent according to claim 21 that is an insecticide.
 24. A harmful organism control agent according to claim 21 having a control effect on a harmful organism in a dry field or a paddy field where a farming or gardening plant is cultured.
 25. A harmful organism control agent according to claim 24, wherein the farming or gardening plant is a plant provided with tolerance by a breeding method or a gene recombination technique.
 26. A method for controlling a harmful organism using an active ingredient amount of the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 3. 27. A method for controlling a harmful organism using an active ingredient amount of the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim
 2. 28. A method for controlling a harmful organism using an active ingredient amount of the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim
 4. 29. A method for controlling a harmful organism by letting a pesticide composition containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof according to claim
 3. 30. A method for controlling a harmful organism by letting a pesticide composition containing the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim 2 as an active ingredient act on a farming or gardening crop or a place where the farming or gardening crop is to be grown or being grown, at once or in batch.
 31. A method for controlling a harmful organism by letting a pesticide composition containing the pyrazole-3-carboxylic acid derivative or an agriculturally acceptable salt thereof according to claim 4 as an active ingredient act on a farming or gardening crop or a place where the farming or gardening crop is to be grown or being grown, at once or in batch.
 32. A method for controlling a harmful organism according to claim 12, wherein the place where the harmful organism control agent is to be applied is a paddy field, a dry field, a lawn, an orchard, a non-crop land, a greenhouse, a raising seeding facility, or a plant factory.
 33. A method for controlling a harmful organism according to any one of claim 12, wherein the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof is used as an insecticide. 